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US 2013 OO17239A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0017239 A1 Viladot Petit et al. (43) Pub. Date: Jan. 17, 2013

(54) LIPID NANOPARTICLE CAPSULES (30) Foreign Application Priority Data (75) Inventors: Josep LLuis Viladot Petit, Barcelona Mar. 24, 2010 (ES) ...... 201030431 (ES); Raquel Delgado Gonzalez, Gava O O Barcelona (ES); Alfonso Fernández Publication Classification Botello, Malaga (ES) (51) Int. Cl. (73) Assignee: LIPOTEC S.A., Gava Barcelona (ES) A 6LX 9/5 (2006.01) (52) U.S. Cl...... 424/401 (21) Appl. No.: 13/636,909 (57) ABSTRACT (22) PCT Filed: Mar. 24, 2011 A delivery system for active ingredients which comprises lipid nanoparticles. Such as Solid lipid nanoparticles (SLN) or (86). PCT No.: PCT/EP11/O1475 nanostructured lipid carriers (NLC), polymerically coated, S371 (c)(1), and their use in the preparation of pharmaceutical, cosmetic (2), (4) Date: Sep. 24, 2012 and/or alimentary compositions. US 2013/001 7239 A1 Jan. 17, 2013

LPDNANOPARTICLE CAPSULES ticle size, level of dispersion of the size, Zeta potential, load efficiency and kinetic release, are determined by the nature of FIELD OF THE INVENTION the lipid matrix, by the mixture of the surfactants, the viscos 0001. This invention relates to a new delivery system for ity of the lipid phase and the aqueous phase at the time of the pharmaceutical, cosmetic and/or alimentary active ingredi emulsion preparation, and also by the general preparation ents which comprises lipid nanoparticles. Such as solid lipid conditions Garzón, M. L. et al. Rev. Mex. Cien. Farm. 39(4): nanoparticles (SLN) or nanostructured lipid carriers (NLC), 50-66 (2008). polymerically coated. 0010. The principal preparation mechanisms of these delivery systems, both SLN and NLC, are: high pressure BACKGROUND OF THE INVENTION homogenization (hot or cold), microemulsion with high speed stirring or ultrasound, emulsion through evaporation or 0002 Solid lipid nanoparticles (SLN) constitute an alter diffusion of the solvent, double emulsion of water in oil in native to other particulate systems for the delivery of active water (w/ofw) or emulsion through a contact membrane ingredients, such as emulsions, liposomes, micelles, micro Uner, M. et al. Int. J. Nanomed. 2: 289-300 (2007); Garzón, particles and/or polymeric nanoparticles. SLN are generated M. L. et al. Rev. Mex. Cien. Farm. 39(4): 50-66 (2008). by substituting the liquid lipid in the emulsions for a solid 0011. The SLN have a solid lipid nucleus which can dis lipid, which means that the SLN are solidat room temperature Solve lipophilic drugs, which is the more common case for as well as at body temperature. use. Examples of stabilized labile lipophilic cosmetic active 0003. The use of SLN as delivery systems enables the use ingredients in SLN would be coenzyme Q10 or retinol of physiologically acceptable lipids, the possibility of avoid Müller, R. H. et al. Adv. Drug Deliv Rev. 54 (Suppl. 1): ing the use of organic solvents in their preparation, and a wide S131-S155 (2002). SLN can also be used with hydrophilic range of routes of administration, which includes through the Substances if they are combined with lipids forming conju skin, orally or intravenously. As well as showing good bio gates: by formation of a salt (with a fatty acid) or by a covalent availability, their principal advantages are: bond (forming or esters with a fatty ) Garzón, 0004. 1. Protection of the active ingredient from chemi M. L. et al. Rev. Mex. Cien. Farm. 39(1): 38-52 (2008). It is cal degradation. The lipid matrix of SLN can protect also possible to incorporate hydrophilic active ingredients in labile active ingredients from hydrolysis and/or oxida the lipid phase of NLC as an aqueous emulsion; this incorpo tion, such as tocopherol, retinol and coenzyme Q10 ration and the Subsequent dispersion of the lipid in the exter Gohla, S. et al. J. Microencapsul. 18:149-158 (2001); nal aqueous phase results in a multiple emulsion system of Schäfer-Korting, M. et al. Adv. Drug Del. Rev. 59: 427 water in oil in water (w/o/w) Müller, R. H. et al. WO 443 (2007). 00/67728A2. 0005 2. Based on the composition of the lipid particles, 0012. The possibility of incorporating peptides in lipid they offer control of the speed of active ingredient particles could constitute a protection of the active ingredient release and therefore the possibility of achieving sus from the proteolytic degradation in the gastrointestinal appa tained release profiles Mehnert, W. et al. Eur: J. Pharm. ratus. However, there are few references of the use of lipids as Biopharm. 45: 149-155 (1998). matrix materials for formulations of peptides and proteins, 0006 3. Control of dehydration of the skin due to an due to, the hydrophobic nature of the lipid matrix, which occlusive effect Müller, R. H. et al. J. Cosm. Sci. 52: makes it more appropriate for incorporating lipophilic active 313-323 (2001). ingredients than hydrophilic proteins. The use of emulsions to 0007 4. According to its components they can act as incorporate hydrophilic active ingredients such as insulin in ultraviolet radiation filters Miller, R. H. et al. Int. J. SLN is described Gallarate, M. et al., J. Microencapsul. 26: Cosm. Sci. 23: 233-243 (2001). 394-402 (2009). In the publication of Gallarate et al. the 0008. A new generation of solid lipid nanoparticles are the preparation method of SLN implies the use of organic sol nanostructured lipid carriers (NLC). These systems have the vents, a factor which is problematic due to the possible reten same advantages as the SLN, and also minimize or avoid tion of their residues. Gasco et al. incorporate thymopentin some possible problems associated with SLN, such as the low pentapeptide in solid lipid nanoparticles by two different loading capacity and active ingredient expulsion during Stor methods: the formation of a lipophilic ion-pair with hexade age. In contrast to the at least partially crystalline State of the cylphosphate, or by the formation of a multiple emulsion lipid phase in SLN, NLC show a less organized solid lipid w/o/w dissolving the peptide in the internal aqueous phase matrix. In the case of NLC, there are both solid and liquid Gasco, M. R. et al. Int. J. Pharm. 132: 259-261 (1996); this compounds in the matrix, thus the greater disorganization latter method is also used by the same authors to incorporate leads to the existence of a greater number of holes with the a polypeptide derived from LHRH in SLN Gasco, M. R. etal. Subsequent increase in the ability to encapsulate active ingre Int. J. Pharm. 105: R1-R3 (1994). Zhou et al. describe an dients. For the preparation of NLC, sterically very different increase in the efficiency of encapsulation and the load capac molecules of lipids are mixed together, mixtures of Solid ity in the incorporation into SLN of different proteins using lipids with liquid lipids or oils Müller, R. H. et al. Adv. Drug PLGA (lactic and glycolic acid copolymer) as an emulsifier Deliv: Rev. 54 (Suppl. 1): S131-S155 (2002). Zhou, W. et al. Colloids and Surfaces, B: Biointerfaces, 67: 0009. The SLN and the NLC are colloidal systems which 199-204 (2008). present the advantages of the liposomes and the microemul 0013 The encapsulation of hydrophilic compounds in sions but are more effective for the protection of the active SLN or NLC presents another problem, as would be the ingredient from chemical degradation and for its controlled diffusion of the active ingredient within the system towards a release. They are 50 to 1000 nm in size and are kept stabilized medium where it would be more soluble, i.e., towards the in an aqueous suspension by hydrophilic Surfactants and aqueous system in which the lipid nanoparticles are in Sus polymers. The principal characteristics of both, such as par pension. US 2013/001 7239 A1 Jan. 17, 2013

0014 NLC and SLN are very suitable vehicles for the ents incorporated into the delivery system of this invention delivery of active ingredients through the skin. Better epider can be, without restriction, cosmetic, pharmaceutical and/or mal penetration of active ingredients is achieved when they alimentary active ingredients and/or adjuvants, among others. are incorporated into SLN or NLC than when they are applied 0022. The lipid nanoparticles in the delivery system con to the skin in the form of a solution or an emulsion. Thus, tain the active ingredients incorporated into their lipid matrix. penetration in the stratum corneum is more effective when an The active ingredients incorporated into lipid matrix can be aqueous dispersion of coenzyme Q10 incorporated into the lipophilic, hydrophilic or amphiphilic, and can be incorpo SLN is applied than when solutions of the active ingredient in rated into the lipid matrix by solution or dispersion in the isopropanol or liquid paraffin are applied. In the same way, in lipid, by adsorption on the surface of the lipid, or by disper vitro studies of epidermal penetration of NLC containing sion of the active ingredient in the lipid in the form of an retinol in comparison with its nanoemulsions, revealed a pen aqueous solution. The active ingredients can be solubilized in etration pattern different over time in both cases, the concen the lipid matrix by addition of surfactants, cyclodextrins or tration of retinol in the skin being greater after 24 hours for the solvents which can optionally be totally or partially elimi formulation which contained NLC Müller, R. H. et al. Adv. nated. When the active ingredient is hydrophilic, it can be Drug Deliv Rev. 54 (Suppl. 1): S131-S155 (2002). incorporated into the system by prior formation of an emul 0015. Among the greatest problems of stability during sion or microemulsion by forming aw/ofw multiple emulsion storage of the SLNSuspensions are the phenomena of gelifi system, or by forming a liposoluble ion pair. cation, aggregation and increase in the size of the particles 0023 Optionally, the delivery system can contain active and expulsion of the drug from the lipid matrix Garzón, M.L. ingredients incorporated into the external aqueous phase of et al. Rev. Mex. Cien. Farm. 39(1): 38-52 (2008). On occa the dispersion. sions, it is advisable to obtain a dry product by atomization or 0024. The polymeric coating of the delivery system of this lyophilization. invention constitutes an additional protection for the active 0016. Although the SLN and the NLC enable the chemical ingredients, increasing their stability against chemical degra stability of the incorporated active ingredients to be dation by interaction with other components of the composi improved, this stabilization is not complete. Surprisingly, the tion, by hydrolysis and/or oxidation due to the presence of authors of this invention have found greater stabilization oxygen and/or light. Furthermore, in the case of hydrophilic against degradation of cosmetic and/or pharmaceutical active active ingredients such as peptides, the loss of the active ingredients incorporated into SLN or NLC when the SLN or ingredient by diffusion towards the external aqueous phase is NLC are polymerically coated. avoided, as usually occurs in the aqueous dispersions of SLN 0017. Furthermore, even though epidermal penetration of or NLC. A greater percutaneous penetration of the active the active ingredients incorporated into SLN or NLC is more ingredients incorporated into the delivery system of the effective than in solution or emulsion, the authors of this invention is also achieved with regards to microemulsions, invention have found that epidermal penetration is still liposomes, SLN or NLC. greater when the SLN or the NLC are polymerically coated, 0025. The preparation processes of the delivery system of and also greater than for liposomes or micelles. this invention consist of two stages: a) preparation of the lipid 0018. This invention proposes a delivery system based on nanoparticles and b) encapsulation of the nanoparticles by lipid nanoparticles. Such as solid lipid nanoparticles (SLN) or polymeric coating, with both stages being able to be carried nanostructured lipid carriers (NLC), polymerically coated, out in a single process. which solves the problems presented by the classic systems 0026. The preparation processes of the lipid nanoparticles described in the prior art. The delivery system of this inven of the delivery system of this invention require, as a prior step, tion avoids the diffusion of hydrophilic active ingredients in obtaining a molten mixture of the lipids by heating to a the SLN and NLC dispersions, enables greater stabilization of temperature higher than that of the melting point of the solid the incorporated active ingredient than in the SLN and the lipids. Next, the lipid nanoparticles can be formed by any of NLC, and has a greater epidermal penetration capacity than the methods described in the literature, preferably by those other known delivery systems. which do not involve the use of organic solvents, such as hot or cold high pressure homogenization Müller, R. H. etal. EP DESCRIPTION OF THE INVENTION 0605497 B2, WO 00/67728A2, Eur: J. Pharm. Biopharm.41: 0019. This invention provides a solution to the aforemen 62-69 (1995); Rehnert et al. Eur: J. Pharm. Biol. 45:149-155 tioned problems. In a first aspect, this invention relates to a (1998), or the microemulsion method Gasco, M. R. et al. new delivery system which comprises lipid nanoparticles, U.S. Pat. No. 5,250,236 A. selected from the group formed by solid lipid nanoparticles 0027. For the preparation of lipid nanoparticles by means (SLN) or nanostructured lipid carriers (NLC), containing at of the hot high pressure homogenization method, the mixture least one active ingredient and which are polymerically of molten lipids, their active ingredients or aqueous emul coated. sions, and optionally emulsifying agents such as Surfactants 0020. The lipid nanoparticles can be found in the form of and coSurfactants, polymers and/or other excipients, are aqueous dispersion inside the delivery system. These lipid emulsified by stirring with a hot aqueous dissolution which nanoparticles are constituted by a solid lipid matrix at room can optionally contain other active ingredients, emulsifiers, temperature, or by a matrix formed by a mixture of liquid polymers and/or other excipients. Subsequently, high pres (oils) and solid lipids at room temperature. The coating on the Sure homogenization is carried out at a temperature higher delivery system constitutes its external part and provides a than the melting points of the lipids. Finally the nanoemulsion complete and continuous coating of the lipid nanoparticles obtained is cooled, obtaining the aqueous dispersion of lipid contained inside. nanoparticles. 0021. The delivery system of this invention contains active 0028. Using the cold homogenization method, the mixture ingredients incorporated into its interior. The active ingredi of molten lipids, their active ingredients or aqueous emul US 2013/001 7239 A1 Jan. 17, 2013

sions, and optionally excipients, is cooled quickly by dry ice 0038. In another particular embodiment, the size of the or liquid nitrogen. Thus the fragility of the lipid is increased capsules of the delivery system of this invention ranges to facilitate the Subsequent grinding process, aimed at obtain between 10 and 10000 nm, preferably between 50 and 5000 ing microparticles of 50-100 m. These microparticles are nm, and more preferably between 100-1000 nm. dispersed in a cold aqueous solution which contains Surfac 0039. The percentage of incorporation of active ingredient tants and which can optionally comprise other active ingre into the delivery system of this invention is quantitative. dients, emulsifiers, polymers and/or other excipients. Finally, 0040. In another particular embodiment, the liquid lipid of the dispersion obtained is Subjected to high pressure homog the delivery system of this invention has a melting point enization at room temperature, or below it. below 4°C., and can be liquid or semi-liquid. The liquid lipid 0029. With the microemulsion method, the mixture of is selected, without restriction, from the group formed by molten lipids, active ingredients, Surfactants, coSurfactants Vegetable oils, such as Soybean oil, Sunflower oil, corn oil, and/or other excipients is microemulsified with hot water olive oil, palm oil, cottonseed oil, colza oil, peanut oil, coco through stirring, and Subsequently dispersed on a cold aque nut oil, castor oil, linseed oil, borage oil, evening primrose oil; ous solution which can optionally contain other active ingre marine oils, such as fish oils and algae oils; oils derived from dients, emulsifiers, polymers and/or other excipients, so the petroleum, Such as mineral oil, liquid paraffin and Vaseline; dispersion of lipid nanoparticles is formed. short-chain fatty alcohols; medium-chain aliphatic branched 0030 The homogenization methods enable smaller lipid fatty alcohols; fatty acid esters with short-chain alcohols, nanoparticles to be obtained and a lower amount of Surfac Such as isopropyl myristate, isopropyl palmitate and isopro tants to be used. pyl Stearate and dibutyl adipate; medium-chain triglycerides 0031. In the case of hydrophilic active ingredients incor (MCT) such as capric and caprylic triglycerides (INCI: porated into a w/o/w multiple emulsion, the size of the inter Capric/caprylic triglycerides) and other oils in the Miglyol(R) nal nanoemulsion drops ranges between 0.1 and 100 nm, series; C2-C octanoates; fatty alcohol ethers, such as dio preferably between 1 and 50 nm, and more preferably ctyl , and/or mixtures thereof. Certain lipophilic active between 10 and 20 nm. ingredients can also act as liquid lipid matrices at room tem 0032. In a particular embodiment, the size of the nanopar perature, for example and not restricted to, beta-carotene, ticles ranges between 1 and 1000 nm, preferably between 10 vitamin E and retinol, and/or mixtures thereof. and 500 nm, and more preferably 100 to 200 nm. 0041. In another particular embodiment, the solid lipid of the delivery system of this invention has a melting point above 0033. In another particular embodiment, in the prepara 37°C. The solid lipid is selected, without restriction, from the tion process of the delivery system of this invention, the group formed by Solid triglycerides, such as trilaurin, trica polymeric coating can be carried out by following the usual prylin, tripalmitin and tristearin, glyceryl trilaurate, glyceryl procedures in the prior art: physical-chemical procedures trimyristate or trimyristin, glyceryl tripalmitate, glyceryl (simple coacervation, complex coacervation, simple or com tristearate, glyceryl behenate or tribehenin; Solid diglycer plex coacervation with pH change during reticulation, evapo ides, such as dipalmitin and distearin; Solid monoglycerides ration of the solvent), chemical procedures (interfacial poly Such as glyceryl monostearate; combinations of glycerides condensation) and mechanical procedures (encapsulation in Such as glyceryl palmitostearate, glyceryl Stearate citrate and an air-fluidized bed). Preferably, the procedure used for the fats of the Witepsol (R) series; long-chain aliphatic alcohols encapsulation of lipid nanoparticles of the delivery system of Such as cetyl alcohol and Stearic alcohol; medium and long this invention is coacervation. chain fatty acids (Co-C) such as Stearic acid, palmitic acid, 0034. When encapsulation is carried out by coacervation, behenic acid and capric acid, and their esters with polyols the procedure can be carried out in a single stage if a solution Such as propylene glycol; fatty alcohol esters of long-chain of the coacervation agent (simple coacervation) or another fatty acids, such as cetyl palmitate, cetearyl olivate and polymer (complex coacervation) is poured onto the disper hydroxyoctacosanyl hydroxyStearate; sterols, cholesteroland sion of nanoparticles under stirring. cholesterol esters such as cholesteryl hemisuccinate, choles 0035. In another particular embodiment, in the formation terylbutyrate and cholesteryl palmitate; fatty amines such as of the polymeric coating of the delivery system of this inven Stearyl amine; waxes such as beeswax, shea butter, cocoa tion a crosslinking agent is used. The crosslinking agent is butter, carnauba wax, oZokerite wax and paraffin wax; cera selected, for example and not restricted to, from the group mides; hydrogenated vegetable oils such as hydrogenated formed by aldehydes, glutaraldehyde, formaldehyde, trans castor oil, quaternary ammonium derivatives, such as behenyl glutaminases, derivatives of methylenebisacrylamide, N.N- trimethyl ammonium chloride (INCI: Alkyltrimethyl ammo methylenebisacrylamide, N,N-(1,2-dihydroxyethylene) nium chloride), and/or mixtures thereof. Certain lipophilic bisacrylamide, derivatives of ethylene glycol dimethacrylate, active ingredients can also act as Solid lipid matrices at room ethylene glycol diacrylate, diethylene glycol diacrylate, tet temperature, for example and not restricted to, Lipochro raethylene glycol diacrylate, ethylene glycol dimethacrylate, man-6 (INCI: Dimethylmethoxy chromanol), Chromabright diethylene glycol dimethacrylate, triethylene glycol (INCI: Dimethylmethoxy chromanyl palmitate), coenzyme dimethacrylate, Sodium tripolyphosphate, N-hydroxysucci Q10 and/or mixtures thereof. namide esters and/or imidoesters. 0042. The percentage of solid lipids is 100% in the SLN; in 0036. In another particular embodiment, the complex the mixtures of lipids of the NLC the liquid lipids and solid coacervation can be carried out with an increase in pH once lipids are mixed in a proportion which ranges between 80:20 the coacervate has been formed and before reticulation, and 0.1:99.9, preferably between 50:50 and 0.1:99.9%, and which enables smaller capsules to be obtained. even more preferably between 30:70 and 0.1:99.9. 0037. The capsules of the delivery system of this invention 0043. The formation of micro- or nanoemulsions requires can be recovered by the usual techniques, such as filtration, the addition of surfactants. In turn, the aqueous dispersions of centrifugation, spray-drying and/or lyophilization. lipid nanoparticles are stabilized by adding Surfactants, US 2013/001 7239 A1 Jan. 17, 2013

coSurfactants, antiflocculants and/or viscosifiers, which favor chloride, benzyl dimethyl hexadecyl ammonium chloride, the formation of nanoparticles at the same time as minimizing distearyl dimethyl ammonium chloride, dilauryl dimethyl the formation of their aggregates. ammonium chloride, dimyristyl dimethyl ammonium chlo ride, , benzalkonium chloride, ben 0044. In another particular embodiment, the surfactant is Zethonium chloride, methyl benzetonium chloride and/or selected from the group formed by nonionic Surfactants, mixtures thereof. amphoteric Surfactants, anionic Surfactants, cationic Surfac tants and/or mixtures thereof. The nonionic Surfactant and/or 0045. In another particular embodiment, the cosurfactant amphoteric Surfactant is selected, without restriction, from is selected, without restriction, from the group formed by the group formed by , alkyl glycosides with an alkyl low-molecular-weight alcohols and glycols, such as pro group that has from 6 to 24 carbon atoms, alkylmaltosides panol, isopropanol, butanol and hexanol; long-chain fatty with an alkyl group that has from 6 to 24 carbon atoms, acids, such as octanoic acid and butyric acid; phosphoric acid ethoxylated alkylphenols with an alkyl group that has from 6 monoesters; benzyl alcohol; biliary acid salts such as sodium to 24 carbon atoms and from 5 to 30 ethylene oxide units, cholate, sodium glycholate, sodium taurocholate, Sodium alkylphenol polyoxyethylene ethers with an alkyl group that taurodesoxycholate and/or mixtures thereof. has from 6 to 24 carbonatoms, Saturated and unsaturated fatty 0046. In another particular embodiment, the antiflocculant alcohols with an alkyl group that has from 8 to 24 carbon is selected, without restriction, from the group formed by atoms, poloxamers, polysorbates, fatty acid esters with Sug Sodium citrate, sodium pirophosphate, sodium Sorbate, ars, Sorbitane esters, polyethylene glycol fatty acid esters, amphoteric Surfactants, cationic Surfactants and/or mixtures castor oil, fatty alcohol and polyoxyethylene ethers, fatty acid thereof. alkanolamides, amine oxides, alkyl betaines with an alkyl 0047. In another particular embodiment, the viscosifier is group that has from 6 to 24 carbon atoms, acyl amido selected, without restriction, from the group formed by cel betaines, alkylsulfobetaines with an alkyl group that has from lulose ethers and esters, such as methyl cellulose, hydroxy 6 to 24 carbon atoms, glycine derivatives, digitonin, inulin ethyl cellulose, hydroxypropyl cellulose and sodium car lauryl carbamate and/or mixtures thereof. More preferably, boxymethyl cellulose; polyvinyl derivatives, such as the nonionic Surfactant and/or amphoteric Surfactant is polyvinyl alcohol, polyvinylpyrrolidone and polyvinyl selected from the group formed by octyl glucoside, decyl acetate; alginates; polyacrylates, Xanthans; pectins and/or glucoside, lauryl glucoside, octyl fructoside, dodecyl malto mixtures thereof. side, decyl maltoside, nonoxynol-9, polyethylene glycol p-(1, 0048. In another particular embodiment, the polymer in 1,3,3-tetramethylbutyl)phenyl ether, palmityl alcohol, oleyl the polymeric coating of the delivery system of this invention alcohol, poloxamer 188, poloxamer 407, polysorbate 20, is selected, without restriction, from the group formed by polysorbate 60, polysorbate 80, methylglucose dioleate, sor proteins, polysaccharides, polyesters, polyacrylates, polycy bitan monostearate or Span 60, Sorbitan monolaurate or Span anoacrylates, copolymers and/or mixtures thereof. Prefer 20, sorbitan monopalmitate or Span 20, sorbitan olivate, ably, the polymeric coating of the microcapsules is selected polyethylene glycol 40 stearate, polyethylene glycol 50 stear from the group formed by gelatin, albumin, soy protein, pea ate, polyethylene glycol 100 Stearate, polyoxyethylene protein, broad bean protein, potato protein, wheat protein, Stearyl ether, polyoxyethylene lauryl ether, cocamide mono whey protein, B-lactoglobulin, caseinates, wheat starch, corn ethanolamine, cocamide diethanolamine, cocamide trietha Starch, Zein, alginates, carrageenans, pectins, arabinogalac nolamine, lauramide diethanolamine, lauramide monoetha tans, gum arabic, Xanthan gum, mesquite gum, tragacanth nolamine, cocamidopropylamine oxide, decyl betaine, gum, galactomannans, guar gum, carob Seed gum, chitosan, dodecyl betaine, tetradecyl betaine, cocoyl betaine, cocami agar, poly(L-lysine), dextran Sulfate sodium, carboxymethyl dopropyl betaine, cocamidopropyl hydroxysultaine, N-2-co galactomannan, carboxymethyl cellulose, methyl cellulose, coylamidoethylhydroxyethylglycinate and N-2-cocoylami ethyl cellulose, hydroxypropyl methyl cellulose (HPMC), doethyl hydroxyethyl carboxy glycinate and/or mixtures cellulose nitrate, cellulose acetate butyrate, cellulose acetate thereof. The anionic surfactant is selected, without restric phthalate, cellulose hydroxypropyl methyl phthalate, cellu tion, from the group formed by Sulfonates such as alkylben lose hydroxypropyl methyl acetate Succinate, polyvinyl Zene Sulfonates, alkyl naphthalene Sulfonates, ethoxylated acetate phthalate, poly(e-caprolactone), poly(p-dioxanone), fatty alcohol Sulfonates, aliphatic Sulfonates, hydroxyalkane poly(Ö-Valerolactone), poly(3-hydroxybutyrate), poly(3-hy Sulfonates, alkyl glyceryl Sulfonate ethers, perfluorooctane droxybutyrate) and p-hydroxyvalerate copolymers, poly(B- Sulfonate; alkyl SulfoSuccinates, alkyl Sulfoacetates; alkyl hydroxypropionate), methylacrylic acid copolymers Sulfates such as Sodium and ammonium lauryl Sulfate, (Eudragit(R) L and S), dimethylaminoethyl methacrylate ethoxylated alkyl sulfates; fatty ester sulfates: ethoxylated copolymers (EudragitR) E), trimethylammonium ethyl meth fatty alcohol Sulfates; alkyl ether Sulfates; acyl isocyanates; acrylate copolymers (Eudragit R. RL and RS), lactic and gly pentafluorooctanoates; carboxylates; ethoxylated alkylphe colic acid polymers and copolymers, lactic and glycolic acid nols; ethanol ammonium salts; diethanolammonium, methy polymers and copolymers and polyethylene glycol and mix lammonium, dimethylammonium, trimethylammonium; tures thereof. alkyl taurates, acyl or fatty acids; alkyl or acyl sarcosinates; 0049. Depending on the properties of the polymer used for phosphates Such as phosphate esters, alkyl phosphates, poly the polymeric coating of the delivery system of this invention, oxyethylene lauryl ether phosphate; glutamates; Stearates; it is possible to increase its specificity. A polymer that pro biliary acids and their salts, such as glycocholic acid and vides the polymeric coating with a positive charge enables the Sodium glycocholate, taurococholic acid and sodium tauro bond of the delivery system of this invention to the hair or cholate, taurodesoxycholate and/or mixtures thereof. The cat textile materials to be increased. Optionally, the polymer in ionic surfactant is selected, without restriction, from the the coating of the delivery system of this invention can be a group formed by quaternary ammonium salts, such as cetyl cationic polymer. The cationic polymer can be a natural or trimethyl ammonium bromide, lauryl trimethyl ammonium synthetic polymer, for example and not restricted to, cationic US 2013/001 7239 A1 Jan. 17, 2013 derivatives of cellulose, Such as quaternized hydroxyethyl silicon dioxide, glycerin, polyethylene glycol, glycerin cellulose, which can be acquired under the name Polymer monostearate and/or metal Stearate salts. JR400TM by Amerchol; cationic starches; diallyl ammonium 0.052 The amount of active ingredient contained in the and acrylamide Salt copolymers; quaternized vinylpyrroli delivery system of this invention ranges between 0.00001 and done/vinylimidazole polymers such as Luviduatt M (BASF); 50% in weight, preferably between 0.0001 and 40% in condensation products of polyglycols and amines; weight, and more preferably between 0.001 and 30% in polyduaternium polymers and copolymers; polymers called weight. polyduaternium-6, polyduaternium-7. polyduaternium-16, 0053. In another particular embodiment, the active ingre polyduaternium-10 Merquats; polyduaternium-4 copoly dient in the delivery system of this invention is selected from mers; dicocoylethylhydroxyethylammonium, grafting the group formed by active ingredients and/or cosmetic and/ copolymers with a cellulose skeleton and quaternary ammo or alimentary adjuvants. In particular, the active ingredients nium groups; quaternized collagen polypeptides such as lau and/or cosmetic and/or alimentary adjuvants are selected, for rdimonium hydroxypropyl hydrolyzed collagen example and not restricted to, from the group formed by (Lamequat TM by Grünau); quaternized wheat polypeptides; Surfactants, humectants or Substances which retain moisture, polyethylenimine; cationic silicone polymers such as ami moisturizers or emollients, agents stimulating healing, coad domethicone or quaternium-22 silicone; adipic acid and dim juvant healing agents, agents stimulating re-epithelialization, ethylamino hydroxypropyl diethylenetriamine copolymers coadjuvant re-epithelialization agents, agents which synthe (CartaretineTM by Sandoz); acrylic acid copolymers with size dermal or epidermal macromolecules, firming and/or dimethyldiallylammonium chloride (MerquatTM 550 by redensifying and/or restructuring agents, cytokine growth Chemviron); cationic chitin derivatives such as chitosan and factors, agents which act on capillary circulation and/or its derivatives; condensation products of cationic dihalogen microcirculation, anti-glycation agents, free radical scaven alkylene such as dibromobutane with bisdialkylamines; bis gers and/or anti-atmospheric pollution agents, reactive car dimethylamino-1,3-; derivatives of cationic guar bonyl species Scavengers, 5C.-reductase-inhibiting agents, gum Such as guar-hydroxypropyltrimonium, JaguarTM CBS, lysyl- and/or prolyl hydroxylase inhibiting agents, defensin JaguarTM C-17, JaguarTM C-16 by Celanese; quaternary synthesis-stimulating agents, bactericidal agents and/or bac ammonium salt polymers such as MirapolTM A-15, teriostatic agents and/or antimicrobial agents and/or germi MirapolTMAD-1, MirapolTMAZ-1 by Miranol; quaternized cidal agents and/or fungicidal agents and/or fungistatic polysaccharide polymers of natural derivatives such as agents and/or germ-inhibiting agents, anti-viral agents, anti azarose; cationic proteins selected from gelatin, gum arabic: parasitic agents, antihistaminic agents, NO-synthase inhibit cationic polymers from the group formed by polyamides, ing agents, descquamation agents or keratolytic agents and/or polycyanoacrylates, polylactides, polyglycolides, polya exfoliating agents, comedolytic agents, anti-psoriasis agents, niline, polypyrrole, polyvinylpyrrolidone, amino silicone anti-dandruff agents, anti-inflammatory agents and/or anal polymers and copolymers, polystyrene, polyvinyl alcohol, gesics, agents, anti-wrinkle and/or anti-aging polystyrene and maleic acid anhydride copolymers, methyl agents, cosmetic and/or absorbent and/or body odor masking vinyl ether, epoxy resins and styrene and methyl methacrylate deodorants, antiperspirant agents, perfuming Substances and/ copolymers; dimethylamino methacrylate, cationic poly or perfumed oils and/or isolated aromatic compounds, anti acrylates and polymethacrylates such as EudragitTMRL 30 D oxidizing agents, agents inhibiting vascular permeability, by Röhm; polyamine derivatives optionally substituted by hydrolytic epidermal enzymes, whitening or skin depigment derivative polyethylene glycol members; polyamino acids ing agents, agents inhibiting Sweat-degrading enzymes, under pH conditions wherein they are cationic; polyethylene agents capable offiltering UV rays, agents which stimulate or imine; quaternized derivatives of polyvinylpyrrolidone regulate keratinocyte differentiation, anti-itching agents, (PVP) and hydrophilic urethane polymers, as well as any agents which stimulate or inhibit the synthesis of melanin, mixture of the aforementioned cationic groups. propigmenting agents, self-tanning agents, agents stimulat ing the proliferation of melanocytes, liquid propellants, Vita 0050. Optionally, the polymer in the coating of the deliv mins, amino acids, proteins, biopolymers, gelling polymers, ery system of this invention can comprise a plasticizing addi skin relaxant agents, agents capable of reducing or treating tive. The plasticizing additive is selected, without restriction, bags under eyes, agents for the treatment and/or care of sen from the group formed by citric acid alkyl esters such as sitive skin, astringent agents, agents regulating sebum pro triethyl citrate, tributyl citrate, acetyl tributyl citrate and duction, anti-stretch mark agents, lipolytic agents or agents acetyl triethylcitrate, phthalates such as butyl phthalate and stimulating lipolysis, Venotonic agents, anti-cellulite agents, diethyl phthalate, glycerin, Sorbitol, maltitol, propylene gly calming agents, agents acting on cell metabolism, agents to col, polyethylene glycol, glucose, saccharose, lanolin, palm improve dermal-epidermal junction, agents inducing hair itic acid, oleic acid, Stearic acid, fatty acid metal salts such as growth or hair-loss retardants, body hair growth inhibiting or Stearic acid or palmitic acid, Sodium Stearate, potassium Stear retardant agents, heat shock protein synthesis stimulating ate, propylene glycol monostearate, acetylated monoglycer agents, muscle relaxants, muscle contraction inhibitory ides such as monoacetylglycerin and glyceryl triacetate or agents, agents inhibiting the aggregation of triacetin, glyceryllecithin, glyceryl monostearate, alkyl seba receptors, agents, elastase inhibitory agents, cates such as dibutyl sebacate or diethyl sebacate, alkyl fuma matrix metalloproteinase inhibitory agents, chelating agents, rates, alkyl Succinates, medium-chain triglycerides (MCT), Vegetable extracts, essential oils, marine extracts, mineral castor oil, hydrogenated vegetable oils, waxes and/or mix salts, cell extracts, emulsifying agents, agents stimulating the tures thereof. synthesis of lipids and components of the stratum corneum 0051 Optionally other technical additives of the polymer (ceramides, fatty acids, etc.), agents obtained from a bio can be added which improve or facilitate the encapsulation fermentation process and/or mixtures thereof. The nature of process such as, for example, fluidizers, such as talc, colloidal these active ingredients and/or cosmetic and/or alimentary US 2013/001 7239 A1 Jan. 17, 2013

adjuvants can be synthetic or natural. Such as Vegetable (Calendula officinalis), jojoba oil (Simmonsis chinensis), extracts, or come from a biotechnological process or from a mango oil (Mangifera indica), avocado oil (Persea gratis combination of a synthetic process and a biotechnological sima), and/or mixtures thereof, among others. process. Additional examples can be found in the CTFA Inter 0055 Likewise, in another particular embodiment, the national Cosmetic Ingredient Dictionary & Handbook, 12th agent stimulating healing, coadjuvant healing agent, agent Edition (2008). In the context of this invention, a biotechno stimulating re-epithelialization and/or coadjuvant re-epithe logical process is understood to be any process which pro lialization agent is selected, for example and not restricted to, duces the active ingredient, or part of it, in an organism, or in from the group formed by extracts of Aristoloquia clematis, a part of it. Centella asiatica, Rosa moschata, Echinacea angustifolia, 0054. In a particular embodiment, the humectant or sub Symphytum officinale, Equisetum arvense, Hypericum perfo stance that retains moisture, moisturizer or emollient is ratum, Mimosa tenuiflora, Persea gratisima, Prunus afri selected, for example and not restricted to, from the group canum, Tormentilla erectea, Aloe vera, Polyplant(R) Epithe formed by polyols and polyethers such as glycerin, ethyl lizing INCI: Calendula Officinalis, Hypericum Perforatum, hexylglycerin, caprylyl glycol, pentylene glycol, butylene Chamomilla Recutita, Rosmarinus Officinalis marketed by glycol, propylene glycol and their derivatives, triethylene Provital, Cytokinol R. LS 9028 (INCI: Hydrolyzed Casein, glycol, polyethylene glycol, Glycereth-26, Sorbeth-30; pan Hydrolyzed Yeast Protein, Lysine HCl marketed by Labora thenol; pyroglutamic acid and its salts and derivatives; amino tories Serobiologiques/Cognis or Deliner(R) INCI: Zea May acids, such as serine, proline, alanine, glutamate or arginine; (Corn) Kernel Extract marketed by Coletica/Engelhard/ ectoine and its derivatives: N-(2-hydroxyethyl)acetamide: BASF, allantoin, cadherins, integrins, selectins, hyaluronic N-lauroyl-pyrrolidone carboxylic acid; N-lauroyl-L-lysine; acid receptors, immunoglobulins, fibroblast growth factor, N--benzoyl-L-arginine; urea; creatine; C- and B-hy connective tissue growth factor, platelet-derived growth fac droxyacids such as lactic acid, glycolic acid, malic acid, citric tor, vascular endothelial growth factor, epidermal growth fac acid or , and their salts; polyglyceryl acrylate; tor, insulin-like growth factor, keratinocyte growth factors, Sugars and polysaccharides, such as glucose, saccharide colony-stimulating factors, transforming growth factor beta, isomerate, Sorbitol, pentaerythritol, inositol. Xylitol, treha tumor necrosis factor alpha, interferons, interleukins, matrix lose and derivatives thereof, sodium glucuronate, carraghen metalloproteinases, receptor protein phosphatases, ates (Chondrus crispus) or chitosan; glycosaminoglycans AntarcticineR INCI: Pseudoalteromonas Ferment Extract. Such as hyaluronic acid and derivatives thereof, aloe Vera in Decorinyl(R) INCI: Tripeptide-10 Citrulline, TrylagenR) any of its forms; honey; soluble collagen; and phos INCI: Pseudoalteromonas Ferment Extract, Hydrolyzed phatidylcholine; ceramides; cholesterol and its esters; toco Wheat Protein, Hydrolyzed Soy Protein, Tripeptide-10 Cit pherol and its esters, such as tocopheryl acetate or tocopheryl rulline, Tripeptide-1, acetyl-glutamyl-methionyl-alanyl-iso linoleate; long-chain alcohols such as cetearyl alcohol, leucine, acetyl-arginyl-phenylglycyl-phenylglycine or stearyl alcohol, cetyl alcohol, oleyl alcohol, isocetyl alcohol acetyl-arginyl-6-aminohexanoyl-alanine marketed by Lipo or octadecan-2-ol; long-chain alcohol esters such as lauryl tec, among others. lactate, myristyl lactate or C-C alkyl benzoates; fatty 0056. In a particular embodiment, the agent stimulating acids such as Stearic acid, isostearic acid or palmytic acid; dermal or epidermal macromolecular synthesis is selected, polyunsaturated fatty acids (PUFAs); sorbitans such as sor for example and not restricted to, from the group formed by bitan distearate; glycerides such as glyceryl monoricinoleate, agents stimulating collagen synthesis, agents stimulating glyceryl monostearate, glyceryl Stearate citrate or caprylic elastin synthesis, agents stimulating decorin synthesis, agents and capric acid triglyceride; saccarose esters such as sac stimulating laminin synthesis, agents stimulating chaperone carose palmitate or saccarose oleate; butylene glycol esters, synthesis, agents stimulating hyaluronic acid synthesis, Such as dicaprylate and dicaprate; fatty acid esters such as agents stimulating aquaporin Synthesis, agents stimulating isopropyl isostearate, isobutyl palmitate, isocetyl Stearate, fibronectin Synthesis, agents inhibiting collagen degradation, isopropyl laurate, hexyl laurate, decyl oleate, cetyl palmitate, agents inhibiting elastin degradation, agents inhibiting serine di-n-butyl sebacate, isopropyl myristate, isopropyl palmitate, proteases Such as leukocyte elastase or cathepsin G, agents isopropyl Stearate, butyl Stearate, butyl myristate, isopropyl stimulating fibroblast proliferation, agents stimulating adipo linoleate, 2-ethylhexyl palmitate, 2-ethylhexylcocoate, decyl cyte proliferation, agents stimulating adipocyte differentia oleate, myristyl myristate; squalene; mink oil; lanolin and its tion, agents stimulating angiogenesis, agents stimulating gly derivatives; acetylated lanolin alcohols; silicone derivatives cosaminoglycan synthesis, DNA repair agents and/or DNA Such as cyclomethicone, dimethicone or dimethylpolysilox protecting agents, for example and not restricted to, extracts ane; AntarcticineR INCI: Pseudoalteromonas Ferment of Centella asiatica, Saccharomyces cerevisiae, Solanum Extract or acetyl-glutamyl-methionyl-alanyl-isoleucine, tuberosum, Rosmarinus officinalis, Vaccinium angustifolium, acetyl-arginyl-phenylglycyl-phenylglycine or acetyl-argi extract of the algae Macrocystis pyrifera, Padina pavonica, nyl-6-aminohexanoyl-alanine marketed by Lipotec, petrola extract of the soy, malt, flax, Sage, red clover, kakkon tum; mineral oil; mineral and synthetic waxes; beeswax (cera to, white lupin, hazelnut extract, corn extract, yeast extract, alba); paraffin, or waxes and oils with vegetable origins such extract of beech tree shoots, extract of leguminosae seeds, as candelilla wax (Euphorbia cerifera), carnauba wax (Co extract of hormones such as gibberellins, auxins or pernicia cerifera), shea butter (Butirospermum parkii), cocoa cytokinins among others, or extract of Zooplankton Salina, butter (Theobroma cacao), castor oil (Ricinus communis), the product of milk fermentation with Lactobacillus Bulgari Sunflower oil (Helianthus annuus), olive oil (Olea europaea), cus, asiaticosides and derivatives thereof, vitamin C and coconut oil (Cocos nucifera), palm oil (Elaeis guineensis), derivatives thereof, cinnamic acid and derivatives thereof, wheat germ oil (Triticum vulgare), Sweet almond oil (Prunus MatrixylR INCI: Palmitoyl Pentapeptide-3, Matrixyl(R) amygdalus dulces), muskrose oil (Rosa moschata), Soya bean 3000 INCI: Palmitoyl Tetrapeptide-3, Palmitoyl Oligopep oil (Glycine soia), grape seed oil (Vitis vinifera), calendula oil tide or Biopeptide CLTMINCI: Glyceryl Polymethacrylate, US 2013/001 7239 A1 Jan. 17, 2013

Propylene Glycol, Palmitoyl Oligopeptide marketed by Sed Coletica/Engelhard, Pepha(R-Timp INCI: Human Oligopep erma, AntarcticineR INCI: Pseudomonas Ferment Extract. tide-20. Regu-Age INCI: Hydrolyzed Rice Bran Protein, Decorinyl(R) INCI: Tripeptide-10 Citrulline, Serilesine(R) Glycine Soja Protein, Oxido Reductases or Colhibin INCI: INCI: Hexapeptide-10, Lipeptide INCI: Hydrolized veg Hydrolyzed Rice Protein marketed by Pentapharm, Lipep etable protein), Aldenine RINCI: Hydrolized Wheat Protein, tide INCI: Hydrolized vegetable protein or Peptide AC29 Hydrolized Soy Protein, Tripeptide-1), Peptide AC29 (INCI: INCI: Acetyl Tripeptide-30 Citrulline marketed by Lipotec, Acetyl Tripeptide-30 Citrulline, acetyl-arginyl-phenylgly LitchidermTM INCI: Litchi Chinensis pericarp extract or cyl-tryptophyl-phenylglycine, acetyl-arginyl-phenylglycyl ArganylTM INCI: Argania Spinosa Leaf Extract marketed valyl-glycine or acetyl-arginyl-phenylglycyl-Valyl-phenylg by Laboratories Serobiologiques/Cognis, MDI Complex(R) lycine marketed by Lipotec, DrielineR PF INCI: Yeast INCI: glycosaminoglycans or ECM-Protect(R) INCI: Water Betaglucan marketed by Alban Muller, Phytovityl CR (Aqua), Dextran, Tripeptide-2 marketed by Atrium Innova INCI: Aqua, Zea Mays Extract marketed by Solabia, Col tions, Dakaline INCI: Prunus amygdalus dulcis, Anogeissus lalift(R) INCI: Hydrolyzed Malt Extract marketed by leiocarpus bark extract marketed by Soliance, Homeostatine Coletica/Engelhard, Phytocohesine(R) PSP proposed INCI: INCI: Enteromorpha compressa, Caesalpinia Spinosamar Sodium Beta-Sitosterol Sulfate marketed by Seporga, min keted by Provital, Timp-Peptide proposed INCI: Acetyl erals such as calcium among others, retinoids and derivatives Hexapeptide or ECM Moduline proposed INCI: Palmitoyl thereof, isoflavonoids, carotenoids, in particular lycopene, tripeptide marketed by Infinitec Activos, IP2000 INCI: pseudodipeptides, retinoids and derivatives thereof Such as Dextran, Trifluoroacetyl tripeptide-2 marketed by Institut retinol or retinyl palmitate among others, or heparinoids Europeen de Biologie Cellulaire, Actimp 1.9.3(R) INCI: among others. Hydrolyzed Lupine Protein marketed by Expanscience 0057. In a particular embodiment, the elastase-inhibiting Laboratories, Vitaderm R) INCI: Alcohol, Water (Aqua), agent is selected, for example and not restricted to, from the Glycerin, Hydrolyzed Rice Protein, Ilex Aquifolium Extract, group formed by Elhibin R) INCI: Glycine Soja (Soybean) Sodium Ursolate, Sodium Oleanolate marketed by Rahn, Protein, PreregenR INCI: Glycine Soja (soybean) Protein, adapalene, and derivatives thereof Such as Oxido Reductases or ReguR-Age INCI: Hydrolyzed Rice , rollitetracycline, , metacycline, Bran Protein, Glycine Soja (Soybean) Protein, Oxido Reduc oxytetracycline, , demeclocycline and their salts, tases marketed by Pentapharm/DSM, Juvenesce INCI: Batimastat BB94: 4-(N-hydroxyamino)-2R-isobutyl-3S Ethoxydiglicol and caprylic Triglycerid, Retinol, Ursolic (thiophene-2-ylthiomethyl)succinyl-L--N- Acid, Phytonadione, Ilomastat, MicromerolTMINCI: Pyrus methylamide, Marimastat BB2516; 2S-N4(R*).2R*, Malus Extract, Heather Extract INCI: Calluna Vulgaris 3S-N42,2-dimethyl-methylaminocarbonylpropyl)-N1, Extract, Extracellium(R) INCI: Hydrolyzed Potato Protein 2-dihydroxy-3-(2-methylpropyl)butanediamide, among or FlavagrumTM PEG INCI: PEG-6 Isostearate, Hesperetin others. Laurate marketed by Coletica/Engelhard/BASF, Proteasyl(R) 0059. In a particular embodiment, the firming and/or TP LS8657 INCI: Pisum Sativum Extract marketed by redensifying and/or restructuring agent is selected, for Laboratoires Serobiologiques/Cognis, acetyl-arginyl-phe example and not restricted to, from the group formed by nylglycyl-tryptophyl-phenylglycine, acetyl-arginyl-phe extracts of Malpighia punicitolia, Cynara scolymus, Gos nylglycyl-Valyl-glycine or acetyl-arginyl-phenylglycyl-va sypium herbaceum, Aloe Barbadensis, Panicum miliaceum, lyl-phenylglycine marketed by Lipotec, Sepilift DPHP Morus nigra, Sesamum indicum, Glycine soia, Triticum vul INCI: Dipalmitoyl hydroxyproline marketed by SEPPIC, gare, Pronalen R. Refirming HSC INCI: Triticum vulgare, Vitaderm R) INCI: Alcohol, Water, Glycerin, Hydrolyzed Silybum Marianum, Glycine Soy, Equisetum Arvense, Rice Protein, Ilex Aquifolium Extract, Sodium Ursolate, Alchemilla Vulgaris, Medicago Sativa, Raphanus Sativus) or Sodium Oleanolate marketed by Rahn, Gatuline(R). Age Polyplant(R) Refirming INCI: Coneflower, Asiatic Centella, Defense 2 INCI: Juglans Regia (Walnut) Seed Extract mar Fucus, Fenugreek marketed by Provital, Lanablue RINCI: keted by Gattefosse, IP2000 INCI: Dextran, Trifluoroacetyl Sorbitol, Algae Extract marketed by Atrium Innovations, Tripeptide-2 marketed by IEB and Atrium, Radicaptol Pepha(R)-Nutrix INCI: Natural Nutrition Factor marketed by INCI: Propylene Glycol, Water, Passiflora Incarnata Flower Pentapharm, or vegetable extracts which contain isoflavones, Extract, Ribes Nigrum (Blackcurrant) Leaf Extract, Vitis Vin Biopeptide ELTM INCI: Palmitoyl Oligopeptide, Biopep ifera (grape) Leaf Extract marketed by Solabia or ViaPureTM tide CLTM INCI: Palmitoyl Oligopeptide, Vexel R. INCI: Boswellia INCI: Olivanum (Boswellia Serrata) Extract Water (Aqua), Propylene Glycol, Lecithin, , Palmi marketed by Soliance, among others. toyl Carnitine, Matrixyl(RINCI: Palmitoyl Pentapeptide-3, 0058. In a particular embodiment, the matrix metallopro Matrixyl R. 3000 INCI: Palmitoyl Tetrapeptide-3, Palmitoyl teinase-inhibiting agent is selected, for example and not Oligopeptide or Bio-BustylTM INCI: Glyceryl Poly restricted to, from the group formed by ursolic acid, isofla methacrylate, Rahnella Soy Protein Ferment, Water (Aqua), Vones such as genistein, quercetin, carotenoids, lycopene, Soy Propylene Glycol, Glycerin, PEG-8, Palmitoyl Oligopeptide extract, cranberry extract, rosemary extract, Trifolium prat marketed by Sederma, Dermosaccharides(RHCINCI: Glyc ense (red clover) extract, Phormium tenax (New Zealand flax) erin, Water (Aqua), Glycosaminoglycans, Glycogen, Agly extract, kakkon-to extract, Sage extract, retinol and deriva cal(R) INCI: Mannitol, Cyclodextrin, Glycogen, Aratosta tives thereof, retinoic acid and derivatives thereof. Sapogenins phylos Uva Ursi Leaf Extract, Cytokinol R. LS INCI: Such as diosgenin, hecogenin, Smilagenin, Sarsapogenin, Hydrolyzed Casein, Hydrolyzed Yeast Protein, Lysine HCLI tigogenin, yamogenin and yucagenin among others, Collal or FirmidermR LS9120 INCI: Terminalia Catappa Leaf ift(R) INCI: Hydrolyzed Malt Extract, Juvenesce INCI: extract, Sambucus Negra Flower Extract, PVP. Tannic Acid Ethoxydiglicol and Caprylic Triglyceride, Retinol, Ursolic marketed by Laboratoires Serobiologiques/Cognis, Liftline(R) Acid, Phytonadione, Ilomastat or EquiStat INCI Pyrus INCI: Hydrolyzed wheat protein), RaffermineR INCI: Malus Fruit Extract, Glycine Soja Seed Extract marketed by Hydrolyzed Soy Flour or Ridulisse C(R) Hydrolyzed Soy US 2013/001 7239 A1 Jan. 17, 2013

Protein marketed by Silab, Serilesine(RINCI: hexapeptide 0063. Likewise, in another particular embodiment, the 10, DecorinylTM INCI: Tripeptide-10 Citrulline, Try lysyl- and/or prolyl-hydroxylase-inhibiting agent is selected, lagenRINCI: Pseudoalteromonas Ferment Extract, Hydro for example and not restricted to, from the group formed by lyzed Wheat Protein, Hydrolyzed Soy Protein, Tripeptide-10 2,4-diaminopyrimidine 3-oxide or 2,4-diamino-6-piperidi Citrulline, Tripeptide-1, marketed by Lipotec, Ursollisome(R) nopyrimidine 3-oxide, among others. INCI: Lecithin, Ursolic Acid, Atelocollagen, Xanthan Gum, 0064. In another particular embodiment, the defensin syn Sodium or Collalift(R) INCI: Hydro thesis-stimulating agent is selected, for example and not lyzed Malt Extract marketed by Coletica/Engelhard, SynR)- restricted to, from the group formed by extracts of or hydro Coll INCI: Palmitoyl Tripeptide-5 marketed by Pentap lyzed Aloe Vera, Roast amaranth, Rehmannias radix, arnica, harm, Hydriame(R) INCI: Water (Aqua), gardenia, carrot, orange, peach, pineapple, mint, gentian, Glycosaminoglycans, Sclerotium Gum marketed by Atrium hibiscus flower, walnut tree leaf, calabaza, peony, quinoa, Innovations or IP2000 INCI: Dextran, Trifluoroacetyl trip boldo, rough bindweed, sunflower, elderberry, seaweed, eptide-2 marketed by Institut Europeen de Biologie Cellu hydrolyzed corn, hydrolyzed soy, hydrolyzed rice, Valine and laire among others. its isomers and derivatives, calcium and its salts, C-MSH and 0060. In a particular embodiment, the anti-glycation agent fragments contained in the amino acid sequence of C-MSH, is selected, for example and not restricted to, from the group Vitamin A and its derivatives and precursors, vitamin D3 and formed by Vaccinium angustifolium extracts, ergothioneine its derivatives, jasmonic acid, fumaric acid, malic acid, citric and derivatives thereof, lysine, Aldenine(RINCI: Hydrolized acid, ascorbic acid, lactic acid, , adipic acid, tar Wheat Protein, Hydrolized Soy Protein, Tripeptide-1. Vilas taric acid, cinnamic acid, glutamic acid, Succinic acid, inulin, teneTM INCI: Lysine HCl, Lecithin, Tripeptide-10 Citrul alkyl glucosides, poly-D-glutamic acid, glycine, L-methion line, dGlyageTM INCI: Lysine HCl, Lecithin, Tripeptide-9 ine, L-alanine, L-citrulline, lactoprotein, casein, lactoperoxi Citrulline or Eyeseryl R. INCI: Acetyl Tetrapeptide-5 mar dase, lysozyme, polyphenol, alkyl glucosides, Lactobacillus keted by Lipotec, hydroxy stilbenes and derivatives thereof, extract, fusobacteria extracts or non-photosynthetic and resveratrol or 3.3',5,5'-tetrahydroxystilbene among others. unfruitful filamentous bacteria, acetyl-glutamyl-methionyl alanyl-isoleucine, acetyl-arginyl-phenylglycyl-phenylgly 0061. In a particular embodiment, the free radical scaven cine oracetyl-arginyl-6-aminohexanoyl-alanine marketed by ger and/or anti-atmospheric pollution agent, and/or the reac Lipotec, among others. tive carbonyl species scavenger is selected, for example and not restricted to, from the group formed by tea extract, olive 0065. In another particular embodiment, the bactericidal leaf extract, Rosmarinus officinalis extract or Eichhornia and/or bacteriostatic agent and/or antimicrobial and/or ger crassipes extract, benzopyrenes, vitamin C and derivatives micidal agent and/or fungicidal agent and/or fungistatic agent thereof, vitamin E and derivatives thereof, in particular toco and/or germ inhibitor is selected, for example and not pherol acetate, ascorbylglycoside, phenols and polyphenols, restricted to, from the group formed by macrollides, pyrano sides, calcium channel blockers, for example and not in particular tannins, tannic acid and ellagic acid, gallocat restricted to, and diltiazem; hormones, for echol, anthocyanins, chlorogenic acid, stilbenes, indoles, cys example and not restricted to, estril, analogues thereof or teine-containing amino acid derivatives, in particular N-ace thyroxine and/or its salts, caprylyl glycol, imidazolidinyl tylcysteine, ergothioneine, S-carboxymethylcysteine, urea, methyl 4-hydroxybenzoate INCI: methylparaben, chelating agents, in particular EDTA or ethylenediamines, ethyl 4-hydroxybenzoate INCI: ethylparaben, propyl 4-hy carotenoids, bioflavonoids, ubiquinone, idebenone, catalase, droxybenzoate INCI: propylparaben, butyl 4-hydroxyben , lactoperoxidase, glutathione peroxi Zoate INCI: butylparaben), isobutyl 4-hydroxybenzoate dase, glutathione, benzylidene camphor, pidolates, lignans, INCI: isobutylparaben), 1,3-bis(hydroxymethyl)-5,5-dim melatonin, oryzanol, carnosine and derivatives thereof, GHK ethylimidazolidine-2,4-dione INCI: DMDM Hydantoin). INCI: Tripeptide-1 and its salts and/or derivatives, Alde benzyl 4-hydroxybenzoate INCI: benzylparaben, benzyl nine(RINCI: Hydrolized wheat protein, hydrolized soy pro alcohol, dehydroacetic acid, benzoic acid, Sorbic acid, Sali tein, tripeptide-1. PreventheliaTM INCI: Diaminopropion cylic acid, formic acid, , 2-bromo-2-nitropro oyl Tripeptide-33 or Lipochroman-6 INCI: pane-1,3-diol, 3-p-chlorophenoxy-1,2-propanodiol INCI: Dimethylmethoxy Chromanol marketed by Lipotec, among chlorphenesin, dichlorobenzyl alcohol, iodopropynylbutyl others. carbamate, benzalkonium chloride, odor-absorbing fungi 0062. In a particular embodiment, the 5C.-reductase inhib cides such as Zinc ricinoleate, cyclodextrins, benzethonium iting agent is selected, for example and not restricted to, from chloride, , ethanol, propanol. 1,3-butanediol. the group formed by extract of Cinnamommun zeylanicum, 1.2-propylene glycol, undecylenic acid, dehydroacetic acid, Laminaria saccharina, Spiraea ulmaria, Nettle Root, N-methylmorpholine acetonitrile (MMA), isopropanol, Pygeum africanum, Avena Sativa, Serenoa repens, extracts of methanol, 1.2-hexanediol. 1.2-octanediol, pentylene glycol, the plants Arnica montana, Cinchona succirubra, Eugenia glycerin laurate, glycerin caprilate, glycerin caprate, benzoyl caryophyllata, Humulus lupulus, Hypericum perforatum, peroxide, chlorhexidine gluconate, triclosan and derivatives Mentha piperita, Rosmarinus officinalis, Salvia officinalis, thereof, phenoxyethanol, terpinen-4-ol, C-terpineol, resorci Thymus vulgaricus, extract of plants of the Silybum, nol, Stiemycin, erythromycin, , clindamycin and its extract of plants which contain Sapogenins and in particular esters, tetracyclines, , azelaic acid, tolnaftate, extract of plants of the genus Dioscorea, retinoids and in nystatin, , ketoconazole, derivatives of Zinc Such particular retinol, sulfur and derivatives thereof, zinc salts and as Zinc piritionate or trithionate, Zinc oxide and Zinc unde in particular lactate, gluconate, pidolate, carboxylate, salicy cylenate, piroctone olamine, isothiazolinones, selenium Sul late or Zinc cysteate, selenium chloride, Vitamin B6, pyridox fur, benzyl hemiformal, boric acid, sodium borate, 6,6-di ine, capryloyl glycine, sarcosine, finasteride, dutasteride, bromo-4,4-dichloro-2,2'-methylenediphenol INCI: iZonsteride, turosteride and their salts, among others. bromochlorophene, 5-bromo-5-nitro-1,3-dioxane, tosyl US 2013/001 7239 A1 Jan. 17, 2013

chloramide sodium INCI: chloramine T. chloroacetamide, pounds such as 4-(2-hydroxyethyl)-1-ethane p-chloro-m-cresol, 2-benzyl-4-chlorophenol INCI: chlo sulfonic acid (HEPES) or sodium methylglycine diacetate rophene, dimethyl oxazolidine, dodecyl dimethyl-2-phe (TRILONRM marketed by BASF); derivatives of 2-oxothia noxyethyl ammonium bromide INCI: , Zolidine-4-carboxylic acid (procysteine); derivatives of Sug 7-ethyl bicyclooxazolidine, , glutaraldehyde, ars such as O-octanoyl-6-D-maltose and N-acetylglu N-(4-chlorophenyl)-N-(4-chloro-3-(trifluoromethyl)phe cosamihe, chestnut extract (Castanea sativa) such as that nyl-urea INCI: cloflucarban, 2-hydroxy-4-isopropyl-2,4, marketed by SILAB under the name Recoverine(R) INCI: 6-cycloheptatriene-1-one INCI: Hinokitiol, isopropylmeth Water (Aqua), Castanea Sativa Seed Extract: opuntia extract ylphenol, mercury salts, aluminum salts, nisin, (Opuntia ficus-indica) such as that marketed by SILAB as phenoxyisopropanol, o-phenylphenol, 3-heptyl-2-(3-hep Exfolactive(R) INCI: Hydrolyzed Opuntia Ficus Indica tyl-4-methyl-3H-thiazole-2-ylidene)methyl-4-methylthiaz Flower Extract; or Phytosphingosine SLC(R) INCI: Salicy ole iodide INCI: Quaternium-73), silver chloride, sodium loyl Phytosphingosine marketed by Degussa/Evonik, Peel iodide, thymol, undecylenic acid, diethylenetriaminepen Moist INCI: Glycerin, Papain, Calcium Pantothenate, Xan taacetic acid, ethylenediaminetetraacetic acid and ethylene than Gum, Caprylyl Glycol, Urea, Magnesium Lactate, diaminetetraacetates, lactoperoxidase, glucose oxidase, Ethylhexylglycerin, Potassium Lactate, Serine, Alanine, Pro lactoferrin, alkylaryl Sulfonates, halogenated phenols, phenol line, Magnesium Chloride, Sodium Citrate; extract or com mercury acetate and/or mixtures thereof, benzamidines, bination of extracts of Saphora japonica, papaya, pineapple, isothiazolines, derivatives of phthalimide, derivatives of pyri squash or yam, and/or mixtures thereof. dine, guanidines, quinolines, 1,2-dibromo-2,4-dicyanobu tane, iodine-2-propylbutyl carbamate, iodine, tamed iodines, 0068. In another particular embodiment, the anti-inflam peroxo compounds, 4-chloro-3,5-dimethylphenol. 2,2'-me matory agent and/or agent is selected, for example thylene-bis(6-bromo-4-chlorophenol), 3-methyl-4-(1-meth and not restricted to, from the group formed by madecassos ylethyl)phenol, 3-(4-chlorophenoxy)-1,2-propanediol. 3.4. ide extract, echinacea extract, amaranth seed oil, sandalwood 4'-trichlorocarbanilide (TTC), thiamine essence, , oil, peach tree leaf extract, extract of Aloe vera, Arnica non farnesol, glycerin monolaurate, diglycerin monocaprinate, tana, Arternisia vulgaris, Asarum maximum, Calendula offi N-alkyl salicylic acid amides such as n-octyl salicylic acid cinalis, Capsicum, Centipeda cunninghamii, Chamomilla amide or n-decyl salicylic acid amide, derivatives of haloge recutita, Crinum asiaticum, Hamamelis virginiana, Harpa nated Xylene and cresol. Such as p-chloro-meta-cresol or gophytum procumbens, Hypericum perforatum, Lilium can p-chloro-meta-xylene, extracts of Allium sativum, Calendula didum, Malva Sylvestris, Melaleuca alternifolia, Origanum officinalis, Chamomilla recutita, Echinacea Purpura, Hysso majorana, Origanum vulgare, Prunus laurocerasus, Ros marinus officialis, Salix alba, Silybum marianum, Tanacetum pus Officinalis, Melaleuca alternifolia or tea tree oil, carna parthenium, Thymus vulgaris, Uncaria guianensis or Vacci tion essence, and mint essence, among others. num myrtillus, mometaSone furoate, prednisolone, nonsteroi 0066. Likewise, in another particular embodiment, the dal antiinflammatories including cyclooxygenase or lipoxy NO-synthase-inhibiting agent is selected, for example and genase inhibitors, , acetylsalicylic acid, not restricted to, from the group formed by extracts of the roSmarinic acid, ursolic acid, derivatives of glycyrrhizinate, plants Vitis vinifera, Olea europaea or Gingko biloba among C.-bisabolol, azulene and analogues, sericoside, ruscogenin, others. escin, scoline, rutin and analogues, hydrocortisone, clobeta 0067. In a particular embodiment, the descquamating agent Sol, , prednisone, , amoxiprin, and/or keratolytic agent and/or exfoliating agent is selected, , salicylate, faislamine, , for example and not restricted to, from the group formed by , , , , hydroxy acids and derivatives thereof, B-hydroxyacids, in , , , indomethacin, oxametha particular salicylic acid and derivatives thereof, or gentisic cin, , , , , dexibupro acid; C.-hydroxyacids and its salts, such as glycolic acid, fen, , , , , ketopro ammonium glycolate, lactic acid, 2-hydroxyoctanoic acid, fen, , , , , C-hydroxycaprylic acid, mandelic acid, citric acid, malic acid , , , , Supro or tartaric acid; C- and B-hydroxybutyric acids; polyhydroxy fen, , meclofenamate, , acids such as gluconic acid, glucuronic acid or saccharic acid; , , , phenylbuta keto acids such as pyruvic acid, glyoxylic acid; pyrrolidin Zone, , , , , ecarboxylic acid; cysteic acid and derivatives; aldobionic , , , Sulfinpyra acids; azelaic acid and derivatives thereof Such as azeloyl Zone, , , , , cele diglycinate; ascorbic acid and derivatives thereof Such as coxib, , , , , Valde 6-O-palmitoylascorbic acid, ascorbylglucoside, dipalmitoy coxib, , , fluproduaZone or licofelone, lascorbic acid, magnesium salt of ascorbic acid-2-phosphate omega-3 and omega-6 fatty acids, , , oxyc (MAP), sodium salt of ascorbic acid-2-phosphate (NAP), odone, , diamorphine, , , ascorbyl tetraisopalmitate (VCIP); nicotinic acid, its esters bupenorphine, benzocaine, lidocaine, chloroprocaine, tetra and nicotinamide (also called vitamin B3 or vitamin PP); caine, procaine, , carbamazepine, gabapentin, nordihydroguaiaretic acid; urea, oligofucoses; cinnamic pregabalin, bisabolol, NeutrazenTM INCI: Water, Butylene acid; derivatives of jasmonic acid; hydroxy stilbenes such as Glycol, Dextran, Palmitoyl Tripeptide-8 marketed by resveratrol; Saccarum officinarum extract; enzymes involved Atrium Innovations/Unipex Group, Meliprene(RINCI: Dex in descquamation or degradation of the corneodesmosomes, tran, Acetyl Heptapeptide-1 marketed by Institut Europeen Such as glycosidases, stratum corneum chymotryptic enzyme de Biologie Cellulaire/Unipex Group, SkinasensylTM INCI: (SCCE) or other proteases Such as trypsin, chymotrypsin, Acetyl Tetrapeptide-15 or AnasensylTM INCI: Mannitol, Sutilain, papain or bromelain; chelating agents such as ethyl Ammonium Glycyrrhizate, Caffeine, Hippocastanum (Horse enediaminetetraacetic acid (EDTA), aminosulfonic com Chestnut) Extract marketed by Laboratoires Serobi US 2013/001 7239 A1 Jan. 17, 2013

ologiques/Cognis, CalmosensineTMINCI: Acetyl Dipeptide 0070. In another particular embodiment, the melanin syn 1 marketed by Sederma, coenzyme Q10 or alkylglycerine thesis stimulating agent, propigmenting agent, self-tanning ethers. agent and/or melanocyte proliferation stimulating agent is selected, for example and not restricted to, from the group 0069. In addition, in another particular embodiment, the formed by extracts of Citrus Aurantium Dulcis Fruit, Coleus whitening or depigmenting agent is selected, for example and forskohli, Coleus Esquirolii, Coleus Scutellariodes, Coleus not restricted to, from the group formed by extracts of Achil Xanthanthus, Ballota nigra, Ballota lanata, Ballota suave lea millefolium, Aloe vera, Aradirachta indica, Asmuna lens, Marrubium cylleneum, Cistus Creticus, Amphiachyris japonica, Autocarpus incisus, Bidens pilosa, Broussonetia amoena, Aster Oharai, Otostegia fruticosa, Plectranthus bar papyrifera, Chlorella vulgaris, Cimicifiuga racemosa, batus, Halinium viscosum or Larix laricema, dihydroxyac Emblica officinalis, Glycyrrhiza glabra, Glycyrrhiza uralen etone and derivatives thereof. Sugars, for example and not sis, Ilex purpurea, Ligusticum lucidum, Ligusticum wallichii, restricted to, erythrulose, melanin and derivatives thereof Mitracarpus scaber, Morinda citrifolia, Morus alba, Morus including melanin polymers and derivatives of melanin with bombycis, Naringi crenulata, Prunus domesticus, Pseudos a low molecular weight which are soluble in water, forskolin tellariae radix, Rumex crispus, Rumex Occidentalis, Sapindus and derivatives thereof including deacetylforskolin and iso mukurossi, Saxifragia sarmentosa, Scutellaria Galericulate, forskolin, tyrosine and derivatives thereof including acetyl Sedum sarmentosum Bunge, Stellaria medica, Triticum Vul tyrosine, oleoyl tyrosine, 3-amino tyrosine and 3-nitroty gare, Uva ursi or Whitania Somnifera, flavonoides, Soy extract, lemon extract, orange extract, ginkgo extract, cucum rosine, copper salts such as CuCl2 carotenoids, canthaxan ber extract, geranium extract, gayuba extract, carob extract, thins, polymers of dihydroxyindole carboxylic acid, 3,4-di cinnamon extract, marjoram extract, rosemary extract, clove hydroxybenzoic acid, 3-amino-4-hydroxybenzoic acid, extract, soluble liquorice extract or blackberry leaf extract, aloin, emodin, alizarin, dihydroxyphenylalanine, 4.5-dihy Lipochroman-6 INCI: Dimethylmethoxy Chromanol or droxynaphthalene-2-sulfonic acid, 3-dimethylaminophenol ChromabrightTM INCI: Dimethylmethoxy Chromanyl or p-aminobenzoic acid, MelatimeTM INCI: Acetyl Tripep Palmitate marketed by Lipotec, ActivhiteTMLS9808 INCI: tide-40 marketed by Lipotec, Heliostatine ISTM INCI: Aqua, Glycerin, Sucrose Dilaurate, Polysorbate 20, Pisum Pisum Sativum Extract marketed by Vincience/ISP. Vegetan sativum (Pea) extract or Dermawhite(R) NF LS9410 INCI: INCI: Dihydroxyacetone or Vegetan Premium INCI: Dihy Mannitol, Arginine HCl, Phenylalanine, Disodium EDTA, droxyacetone, Melanin marketed by Soliance, Melano Sodium Citrate, Kojic Acid, Citric Acid, Yeast Extract mar Bronze INCI: Vitex Agnus Castus Extract, Acetyl Tyrosine keted by Laboratoires Serobiologiques/Cognis, LumiskinTM marketed by Mibelle Biochemistry, Melitane(RINCI: Acetyl INCI: Caprylic/Capric Triglycerid, Diacetyl-Boldine, Hexapeptide-1 marketed by Institut Europeen de Biologie MelaclearTM INCI: Glycerin, Aqua, Dithiaoctanediol, Glu Cellulaire/Unipex Innovations, Actibronze(R) INCI: Hydro conic acid, Sutilains, Beta-carotene, O.D.A.whiteTMINCI: lyzed Wheat Protein, Acetyl Tyrosine, Copper Gluconate or octadecendioic acid or EtiolineTMINCI: Glycerin, Butylene Instabronze(RINCI: Dihydroxyacetone, Tyrosine marketed Glycol, Arctostaphylos uva ursi Leaf Extract, Mitracarpus by Alban Muller, Thalitan INCI: Hydrolyzed Algin, Magne scaber Extract marketed by Sederma, SepiwhiteTM MSH sium Sulfate, Manganese Sulfate marketed by CODIF, INCI: Undecylenoyl Phenylalanine marketed by Seppic, Tyrosilane(R) INCI: Methylsilanol Acetyltyrosine marketed Achromaxyl INCI: Aqua, Brassica napus Extract marketed by ExSymol, Tyr-ExcelTM INCI: Oleoyl Tyrosine, Luffa by Vincience, GigawhiteTM INCI: Aqua, Glycerin, Malva Cylindrica Seed Oil, Oleic Acid or Tyr-Ol INCI: Oleoyl Sylvestris (Mallow) Extract, Mentha piperita Leaf Extract, Tyrosine. Butylene glycol, Oleic Acid marketed by Sed Primula veris Extract, Alchemilla vulgaris Extract, Veronica erma/Croda, Bronzing S.F. proposed INCI: Butiryl Pen officinalis Extract, Melissa officinalis Leaf Extract, Achillea tapeptide marketed by Infinitec Activos or Biotanning R millefolium Extract, Melawhite RINCI: Leukocyte Extract, INCI: Hydrolyzed Citrus Aurantium Dulcis Fruit Extract AHA or Melfade R-J INCI: Aqua, Arctostaphylos uva-ursi marketed by Silab, among others. Leaf Extract, Glycerin, Magnesium Ascorbyl Phosphate 0071. In a particular embodiment, the anti-wrinkle and/or marketed by Pentapharm, AlbatinRINCI: Aminoethylphos anti-aging agent is selected, for example and not restricted to, phoric Acid, Butylene Glycol, Aqua marketed by ExSymol, from the group formed by extracts of Vitis vinifera, Rosa Tyrostatt M-11 INCI: Aqua, Glycerin, Rumex occidentalis canina, Curcuna longa, Iris paffida, Theobroma cacao, Extractor Melanostatine(R)-5 INCI: Dextran, Nonapeptide Ginkgo biloba, Leontopodium Alpinum or Dunaliella salina, 1 marketed by Atrium Innovations, arbutin and its isomers, MatrixylR INCI: Palmitoyl Pentapeptide-4, Matrixyl kojic acid and derivatives thereof, ascorbic acid and deriva 3000.R INCI: Palmitoyl Tetrapeptide-7, Palmitoyl Oli tives thereof such as 6-O-palmitoylascorbic acid, ascorbyl gopeptide, EssenskinTM INCI: calcium hydroxymethion glucoside, dipalmitoylascorbic acid, magnesium salt of ine, Renovage INCI: teprenone or DermaxylR INCI: ascorbic acid-2-phosphate (MAP), sodium salt of ascorbic Palmitoyl Oligopeptide marketed by Sederma, VialoxR) acid-2-phosphate (NAP), ascorbyl glucoside or ascorbyl tet INCI: Pentapeptide-3), Syn R-Ake(R) INCI: Dipeptide raisopalmitate (VCIP); retinol and derivatives thereof includ Diaminobutyroyl Benzylamide Diacetate, SynR-Coll ing tretinoin and isotretinoin, idebenone, hydroxybenzoic INCI: Palmitoyl Tripeptide-5), Phytaluronate INCI: Locust acid and derivatives thereof, niacinamide, liquiritin, resorci Bean (Ceratonia Siliqua) Gum or PreregenRINCI: Glycine nol and derivatives thereof, hydroquinone, C-tocopherol, Soja (Soybean) Protein, Oxido Reductases marketed by Pen Y-tocopherol, azelaic acid, azeloyl diglycinate, resveratrol, tapharm/DSM, MyoxinolTM INCI: Hydrolyzed Hibiscus linoleic acid, C.-lipoic acid, dihydrolipoic acid, C-hydroxy Esculentus Extract. SyniorageTM INCI: Acetyl Tetrapep acids, B-hydroxy acids, ellagic acid, ferulic acid, cinnamic tide-11, DermicanTM INCI: Acetyl Tetrapeptide-9 or DN acid, oleanolic acid, aloesin and its derivatives and/or serine AGETMLS INCI: Cassia Alata leaf Extract marketed by protease inhibitors, for example and not restricted to, Laboratoires Serobiologiques/Cognis, Algisum C(R) INCI: tryptase, trypsin or PAR-2 inhibitors, among others. Methylsilanol Mannuronate or Hydroxyprolisilane CNR) US 2013/001 7239 A1 Jan. 17, 2013

INCI: Methylsilanol Hydroxyproline Aspartate marketed Myrrha, Crithmum Maritimum, Eugenia Caryophyllus, by Exsymol, Argireline(R) INCI: Acetyl Hexapeptide-8. Ginkgo Biloba, Hedera Helix (ivy extract), Hibiscus Sabdar SNAP-7 INCI: Acetyl Heptapeptide-4, SNAP-8 INCI: ifa, Ilex Paraguariensis, Laminaria Digitata, Nelumbium Acetyl Octapeptide-3, Leuphasyl(R) INCI: Pentapeptide Speciosum, Paulinia Cupana, Peumus Boldus, Phyllacantha 18, Aldenine(RINCI: Hydrolized wheat protein, hydrolized Fibrosa, Prunella Vulgaris, Prunus Amygdalus Dulcis, Rus soy protein, Tripeptide-1. PreventheliaTM INCI: Diamino cus Aculeatus (Butcherbroom extract), Sambucus Nigra, propionoyl Tripeptide-33), DecorinylTM INCI: Tripeptide Spirulina Platensis Algae, Uncaria Tomentosa or Verbena 10 Citrulline. TrylagenR INCI: Pseudoalteromonas Fer Officinalis, dihydromyricetin, coenzyme A, lipase, , ment Extract, Hydrolyzed Wheat Protein, Hydrolyzed Soy esculin, visnadine, ReguR-Shape INCI: Isomerized Linoleic Protein, Tripeptide-10 Citrulline, Tripeptide-1. Eyeseryl(R) Acid, Lecithin, Glycerin, Polysorbate 80 marketed by Pen INCI: Acetyl Tetrapeptide-5), Peptide AC29 (INCI: Acetyl tapharm/DSM, UCPeptideTM V INCI: Pentapeptide or AT Tripeptide-30 Citrulline, Lipochroman-6 INCI: Dimethyl PeptideTM IS INCI: Tripeptide-3 marketed by Vincience? methoxy Chromanol, ChromabrightTM INCI: Dimethyl ISP, Liporeductyl RINCI: Caffeine, Butcherbroom (Ruscus methoxy Chromanyl Palmitate, Antarcticine(R) INCI: Aculeatus) Root Extract, TEA-Hydroiodide, Carnitine, Ivy Pseudoalteromonas Ferment Extract, VilasteneTM INCI: (Hedera Helix) Extract, Escin, Tripeptide-1 marketed by Lysine HCl, Lecithin, Tripeptide-10 Citrulline, dGlyageTM Lipotec, Adiposlim INCI: Sorbitan Laurate, Lauroyl Pro INCI: Lysine HCl, Lecithin, Tripeptide-9 Citrulline, acetyl line marketed by SEPPIC, caffeine, carnitine, escin and/or arginyl-phenylglycyl-tryptophyl-phenylglycine, acetyl-argi triethanolamine iodide, among others. nyl-phenylglycyl-Valyl-glycine or acetyl-arginyl-phenylgly 0073. In a particular embodiment, the heat shock protein cyl-valyl-phenylglycine, InylineTM INCI: Acetyl synthesis stimulating agent is selected, for example and not Hexapeptide-30 marketed by Lipotec, KollarenR INCI: restricted to, from the group formed by extracts of Opuntia Tripeptide-1, Dextran marketed by Institut Europeen de ficus indica, Salix alba, Lupinus spp., Secale cereale, extracts Biologie Cellulaire, Collaxyl(R) IS INCI: Hexapeptide-9), ofred algae from the genus Porphyra, extracts of crustaceans Laminixyl ISTM INCI: Heptapeptide, OrsirtineTM GL from the genus Artemia, jojoba seed oil, grape seed extracts, INCI: Oryza Sativa (Rice) Extract, D'OrientineTMISINCI: green tea extracts, geranylgeranylacetone, celastrol, Zinc and Phoenix Dactylifera (Date) Seed Extract. Phyto its salts, 2-cyclopenten-1-one, proteasome inhibitors, for quintescineTM INCI: Einkorn (Triticum Monococcum) example and not restricted to, bortezomib; and Extract or QuintescineTM IS INCI: Dipeptide-4 marketed derivatives thereof, hydroxylamine and derivatives thereof, by Vincience/ISP BONT-L-Peptide INCI: Palmitoyl for example and not restricted to, bimoclomol; chalcone and Hexapeptide-19 marketed by Infinitec Activos, DeepalineTM derivatives thereof, hyperosmotic agents, for example and not PVBINCI: Palmitoyl hydrolyzed Wheat Protein or Sepil restricted to, sorbitol and derivatives thereof, mannitol and ift(R) DPHP INCI: Dipalmitoyl Hydroxyproline marketed derivatives thereof or glycerol and derivatives thereof, isos by Seppic, Gatuline(R) Expression INCI: Acmella oleracea orbide, urea or salicylic acid and derivatives thereof among Extract, Gatuline(R). In-Tense INCI: Spilanthes Acmella others, or mixtures thereof. Flower Extractor Gatuline.R Age Defense 2 INCI: Juglans 0074. In a particular embodiment, the hair growth induc Regia (Walnut) Seed Extract marketed by Gattefossé, ing or hair loss retardantagentis selected, for example and not ThalassineTMINCI: Algae Extract marketed by Biotechma restricted to, from the group formed by the extracts of Tussi rine, ChroNOlineTM INCI: Caprooyl Tetrapeptide-3 or lago farfara or Achillea millefolium, nicotinic acid esters Thymulen-4 INCI: Acetyl Tetrapeptide-2 marketed by such as C-C alkyl nicotinates such as methyl or hexyl nico Atrium Innovations/Unipex Group. EquiStat INCI: Pyrus tinate, benzyl nicotinate, or tocopheryl nicotinate; biotin, Malus Fruit Extract, Glycine Soja Seed Extractor Juvenesce 5C-reductase-inhibiting agents, anti-inflammatory agents, INCI: Ethoxydiglicol and Caprylic Triglycerid, Retinol, retinoids, for example and not restricted to, All-trans-retinoic Ursolic Acid, Phytonadione, Ilomastat marketed by acid ortretinoin, isotretinoin, retinol or vitaminA, and deriva Coletica, Ameliox. INCI: Carnosine, Tocopherol, Silybum tives thereof. Such as acetate, palmitate, propionate, motre Marianum Fruit Extract or PhytoCellTec Malus Domestica tinide, etretinate and Zinc salt of trans-retinoic acid; anti INCI: Malus Domestica Fruit Cell Culture marketed by bacterial agents, calcium channel blockers, for example and Mibelle Biochemistry, Bioxilift INCI: Pimpinella Anisum not restricted to, cinnarizine and diltiazem; hormones, for Extract or SMS Anti-WrinkleR INCI: Annona Squamosa example and not restricted to, estriol, its analogues orthyroX Seed Extract marketed by Silab, Ca" channel blockers, for ine, its analogues and/or salts; antiandrogenic agents, for example and not restricted to, alverin, manganese or magne example and not restricted to, Oxendolone, spironolactone or sium salts, certain secondary or tertiary amines, retinol and diethylstilbestrol; anti-radical agents, esterified oligosaccha derivatives thereof, resveratrol, idebenone, coenzyme Q10 rides, for example and not restricted to, those described in and derivatives thereof, boswellic acid and derivatives documents EP 0211610 and EP 0064.012; derivatives of hex thereof, GHK and derivatives thereof and/or salts, carnosine asaccharide acids, for example and not restricted to, glucose and derivatives thereof, DNA repair enzymes, for example saccharide acid or those described in document EP 0375388; and not restricted to, photolyase or T4 endonuclease V, or glucosidase inhibitors, for example and not restricted to, chloride channel blockers among others. D-glucaro-1,5-lactam or those described in document EP 0072. In a particular embodiment, the lipolytic agent or 0334586; glycosaminoglycanase and proteoglycanase agent stimulating lipolysis, Venotonic agent and/or anti-cel inhibitors, for example and not restricted to L-galactono-1,4- lulite agent is selected, for example and not restricted to, from lactone or those described in document EP 0277428; tyrosine the group formed by extracts of Bupleurum Chinensis, Cecro kinase inhibitors, for example and not restricted to, 1-amido pia Obtusifolia, Celosia Cristata, Centella Asiatica, Che 1-cyano(3,4-dihydroxyphenyl)ethylene or those described nopodium Ouinoa, Chrysanthellum Indicum, Citrus Auran in, document EP 0403238, diazoxides, for example and not tium Amara, Coffea Arabica, Coleus Forskohlii, Commiphora restricted to, 7-(acetylthio)-4',5'-dihydrospiro.androst-4- US 2013/001 7239 A1 Jan. 17, 2013

ene-17,2'-(3H) furan-3-one, 1,1-dioxide of 3-methyl-7- probucol, polyphenoles, ascorbic acid and its salts, enzymes chloro2H-1,2,4-benzothiadiazine or spirooxazine; phos Such as catalase, Superoxide dismutase and peroxidases; cit pholipids, for example and not restricted to, lecithin; salicylic ric acid, citrates, monoglyceride esters, calcium metabisul acid and derivatives thereof, hydroxycarboxylic or keto car fate, lactic acid, malic acid, Succinic acid, tartaric acid, Vita boxylic acid and esters thereof, lactones and their salts; min A or B-carotene, Vitamins E and C, tocopherols such as anthralin, eicose-5,8,11-trienoic acids and esters thereof or Vitamin Eacetate, ascorbic acid esters such as ascorbyl palmi amides among others, minoxidil and derivatives thereof or tate and ascorbyl acetate, Zinc, copper, mannitol, reduced mixtures thereof. glutathione, carotenoids such as cryptoxanthin, astaxanthin 0075. In another particular embodiment the body hair and lycopene; cysteine, uric acid, carnitine, taurine, tyrosine, growth inhibiting or retardant agent is selected, for example lutein, Zeaxanthin, N-acetyl-cysteine, carnosine, Y-glutamyl and not restricted to, from the group formed by activin or cysteine, quercetin, lactoferrin, dihydrolipoic acid, tea cat activin , flavonoids such as quercetin, curcumin, echins, retinyl palmitate and derivatives thereof, bisulfate, galangin, fisetin, myricetin, apigenin, propyl gallate, nordi metabisulfite and Sodium sulfite, chromans, chromens and hydroguaiaretic acid, caffeic acid, tyrosine kinase inhibitors their analogues, Lipochroman-6 INCI: Dimethylmethoxy Such as lavendustin, erbstatin, tyrphostins, benzoquinone Chromanol, chelating agents of metals such as EDTA, Sor ansamycin herbimycin A, thiazolidinediones, , bitol, phosphoric acid ordGlyageTMINCI: Lysine HCl, Leci 2,3-dihydro-2-thioxo-1H-indol-3-alcanoic acids, phenothi thin, Tripeptide-9 Citrulline; extract of Ginkgo Biloba, plant azine derivatives such as ; sphingosine and extracts Such as sage, pomegranate, rosemary, oregano, gin derivatives thereof, staurosporine and derivatives thereof, ger, marjoram, cranberry, grape, tomato, green tea or black glycyrrhetinic acid, lauryl isoquinolinium bromide, Dece tea; oleoresin extract, extract of plants which contain phenols lerineTMINCI: Lauryl Isoquinolium Bromide, Pseudoaltero Such as Vanillin, ellagic acid and resveratrol; tertiary butyl monas Ferment Extract marketed by Lipotec or serine pro hydroquinone or mixtures thereof, metal salts with a valence tease inhibitors, trypsin and/or mixtures thereof. of 2 such as selenium, cadmium, Vanadium or Zinc, C-lipoic 0076. In a particular embodiment, the cosmetic and/or acid, coenzyme Q, idebenone or derivatives thereof. absorbent and/or body odor masking deodorant and/or anti 0078. In a particular embodiment, the agent inhibiting perspirant agent, perfuming Substance and/or perfumed oil is Sweat-degrading enzymes is selected, for example and not selected, for example and not restricted to, from the group restricted to, from the group formed by trialkyl citrates such formed by the complex zinc salt of ricinoleic acid, Styrax, as trimethyl citrate, tripropyl citrate, triisopropyl citrate, derivatives of abiotic acid, sage essence, chamomile essence, tributyl citrate or triethylcitrate; lanosterine sulfate or phos carnation essence, lemon balm essence, mint essence, cinna phate, cholesterin, campesterin, Stigmasterin and sitosterin; mon leaf essence, lime flower essence, juniperberry essence, dicarboxylic acids and their esters, such as glutaric acid, Vetiver essence, olibanum essence, galbanum essence, lab monoethyl glutarate, diethyl glutarate, adipic acid, monoet danum essence, lavender essence, peppermint essence, ber hyl adipate, diethyl adipate; malonic acid and diethyl mal gamot orange, dihydromyrcenol, lilial, lyral, citronellol, onate, hydroxycarboxylic acids and their esters such as malic lemon essence, mandarin essence, orange essence, lavender acid, tartaric acid or diethyl tartrate, Zinc glycinate and/or essence, muscat, geranium bourbon essence, aniseed, mixtures thereof. cilantro, cumin, juniper, extracts of fleur-de-lis, lilac, roses, 0079. In another particular embodiment, the agent capable jasmin, bitter orange blossom; benzyl acetate, p-tert-butylcy offiltering UV rays is selected, for example and not restricted clohexyl acetate, linallyl acetate, phenylethyl acetate, ethylm to, from the group formed by organic or mineral photopro ethylphenylglycinate, linallylbenzoate, benzyl formate, allyl tective agents active against A and/or B ultraviolet rays Such cyclohexyl propionate, styrallyl propionate, benzyl salicy as substituted benzotriazoles, substituted diphenylacrylates, late, benzyl ethyl ether, linear alkanes with from 8 to 18 organic nickel complexes, umbelliferone, urocanic acid, carbon atoms, citral, ricinoleic acid, citronellal, citronellyl biphenyl derivatives, stilbene, 3-benzylidene camphor, and oxyacetaldehyde, cyclamen aldehyde, hydroxycitronellal, derivatives thereof such as 3-(4-methylbenzylidene)cam bourgeonal, ionones, methyl cedryl ketone, anethole, phor; derivatives of 4-aminobenzoic acid, 2-ethylhexyl eugenol, isoeugenol, geraniol, linalool, terpineol, phenyl 4-(dimethylamino)benzoate, 2-octyl 4-(dimethylamino)ben ethyl alcohol, C.-hexylcinnamaldehyde, geraniol, benzylac Zoate and amyl 4-(dimethylamino)benzoate, cinnamic acid etone, cyclamen aldehyde, Boisambrene Forte R, ambroxan, esters, such as 2-ethylhexyl 4-methoxycinnamate or diethy indole, hedione, Sandelice, cyclovertal, B-damascone, allyl lamino hydroxybenzoylhexylbenzoate, propyl 4-methoxy amylglycolate, dihydromyrcenol, phenoxyethyl isobutyrate, cinnamate, isoamyl 4-methoxycinnamate, 2-ethylhexyl (oc cyclohexyl salicylate, Vertofix Coeur, Iso-E-Super, Fixolide tocrylenes) 2-cyano-3,3-phenyl cinnamate; salicylic acid NP. Evernyl, phenylacetic acid, geranyl acetate, romillat, iro esters, such as 2-ethylhexyl salicylate, 4-isopropylbenzyl tyl, floramate, active astringent products such as aluminum salicylate, homomethyl salicylate; benzophenone deriva chloride, aluminum chlorohydrate, aluminum dichlorohy tives, such as 2-hydroxy-4-methoxybenzophenone, 2-hy drate, aluminum sesquichlorohydrate, aluminum hydroxyal droxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy lantoinate, aluminum chlorotartrate, aluminum and Zirco 4-methoxybenzophenone; benzalmalonic acid esters, such as nium trichlorohydrate, aluminum and Zirconium di-2-ethylhexyl 4-methoxybenzalmalonate; triazine deriva tetrachlorohydrate, aluminum and Zirconium pentachlorohy tives, such as 2.4.6-trianilino, p-carbo-2'-ethyl-1-hexyloxy-1, drate and/or mixtures thereof. 3,5-triazine, octyl triazone or dioctyl butamido triazones: 0077. In a particular embodiment, the antioxidant is propane-1,3-diones, such as 1-(4-tert-butylphenyl)-3-(4- selected, for example and not restricted to, from the group methoxyphenyl)propane-1,3-dione; ketotricyclo(5.2.1.0)de formed by butylhydroxytoluene (BHT), butylhydroxyanisole cane derivatives; 2-phenylbenzimidazole-5-sulfonic acid; (BHA), tert-butylhydroquinone (TBHQ), 2.6,-di-tert-butyl benzophenone Sulfonic acid derivatives, such as 2-hydroxy 4-methylphenol, gallic acid esters such as propyl gallate, 4-methoxybenzophenone-5-Sulfonic acid and its salts, 4-(2- US 2013/001 7239 A1 Jan. 17, 2013 oxo-3-bornylidenemethyl)benzenesulfonic acid, benzoyl I0083. In particular, the pharmaceutical active ingredients methane derivatives, such as benzoyl methane 2-methyl-5- and/or adjuvants are selected, for example and not restricted (2-oxo-3-bornylidene)sulfonic acid, such as 1-(4'-tert-bu to, from the group formed by antiacids, agents against peptic tylphenyl)-3-(4-methoxyphenyl)propane-1,3-dione, 4-tert ulcers and gastroesophageal reflux disease, antispasmodics, butyl-4'-methoxydibenzoylmethane, 1-phenyl-3-(4- , anticholinergic drugs, propulsive drugs, antiemet isopropylphenyl)-propane-1,3-dione, enamine compounds, ics, antinausea drugs, agents for biliary therapy, agents for anthranilates, silicons, benzimidazole derivatives, imidazo hepatic therapy, lipotropics, laxatives, antidiarrhetics, intes lines, benzoyl derivatives, ChromabrightTM INCI: Dimeth tinal adsorbents, antipropulsives, anti-inflammatory drugs, ylmethoxy Chromanyl Palmitate or PreventheliaTM INCI: active ingredients against obesity, enzymes, hypoglycemic Diaminopropionoyl Tripeptide-33 both marketed by Lipo drugs, insulin and analogues, vitamins, proteins, minerals, tec, metal oxides Such as Zinc oxide, titanium, iron, Zirco anabolic steroids, antithrombotic agents, antifibrinolytics, nium, silicon, manganese, aluminum and cerium; silicates, haemostatic agents, antiarrhythmic agents, cardiac stimu talc, barium Sulfate, Zinc Stearate, carbon nanotubes and/or lants, cardiac glycosides, vasodilators, antiadrenergic agents, mixtures thereof. antihypertensive drugs, diuretics, potassium-saving agents, 0080. In addition, in another particular embodiment, the antihemorrhoidals, antivaricose therapy agents, capillary sta agent stimulating or regulating keratinocyte differentiation is bilizing agents, agents which act on the renin-angiotensin selected, for example and not restricted to, from the group system, beta-blockers, selective calcium-channel blockers, formed by minerals such as calcium, retinoids such as retinol non-selective calcium-channel blockers, ACE inhibitors, or tretinoin, analogues of vitamin D3 Such as calcitriol, cal angiotensin II inhibitors, agents modifying lipids, antifun cipotriol or tacalcitol, lupine (Lupinus albus) extract such as gals, healing agents, antipruritics, antihistamines, anesthet that marketed by SILAB under the name StructurinRINCI: ics, antipsoriatics, chemotherapy drugs, , anti Hydrolyzed Lupine Protein). B-sitosterol sulfate, such as that septics, disinfectants, anti-acne agents, products for marketed by Vincience/ISP under the name Phytocohesine gynecological use, oxytocics, anticonceptives, androgen, PSPR INCI: Sodium Beta-sitosterol Sulfate, maize (Zea estrogen, progestagen, ovulation , gonadotropins, Mays) extract such as that marketed by Solabia under the antiandrogens, products for urological use, antispasmodics, name Phytovityl CR INCI: Water (Aqua), Zea Mays drugs used in benign prostatic hypertrophy, hormones, hor Extract. Helix Aspersa Miller glycoconjugates and/or mix mone antagonists, , tetracyclines, anphenicols, tures thereof. beta-lactam antibacterials, penicillin, Sulfonamides, trime 0081 Likewise, in another particular embodiment, the thoprim, macrollides, lincosamides, streptogramins, antibac , agent inhibiting muscle contraction, agent terial aminoglycosides, antibacterial quinolones, antivirals, inhibiting clustering and/or anticho immune serum, immunoglobulins, antineoplastic agents, linergic agent is selected, for example and not restricted to, immunomodulatory agents, alkylation agents, antimetabo from the group formed by extracts of , lites, plant and other natural products, cytotoxic , Mandragora officinarum, Chondoden antibiotics, immunosuppressive agents, drugs for disorders of dron tomehtosum, plants of the genus, or the the musculoskeletal system, antirheumatics, muscle relaxant genus, Clostridium botulinum toxin, peptides derived agents, agents which affect bone structure and mineraliza from the protein SNAP-25 or InylineTM INCI: Acetyl tion, drugs which act on the nervous system, general anes Hexapeptide-30 marketed by Lipotec, baclofen, carbidopa, thetics, local , , antimigraine agents, anti levodopa, , chlorphenesin, chlorZoxazone, convulsants, anticholinergic agents, dopaminergic agents, donepezil, mephenoxalone, reserpine, tetrabenazine, dant antipsychotics, anxiolytics, hypnotics, sedatives, antidepres rolene, , tizanidine, clonidine, , sants, psychoStimulants, anti-dementia drugs, parasympatho glycopyrrolate, , , benztropine, Scopo mimetics, drugs used in addictive disorders, anti-vertigo lamine, , , , agents, antiparasitic agents, insecticides, insect repellants, dicyclomine, , , , nasal , mucolytic agents, cough Suppressants, , ipratropium, , , tiotro ophthalmic active ingredients, otological active ingredients, pium, , , , , antiglaucoma drugs, miotics, mydriatics, cycloplegics and/or , , trimethaphan, atracurium, cisatra mixtures thereof. curium, doxacurium, faZadinium, , mivacurium, I0084. The delivery system of this invention can also be pancuronium, pipecuronium, rapacuronium, tubocuranine, adsorbed on Solid organic polymers or Solid mineral Supports, dimethyl tubocuranine, rocuronium, Vecuronium, SuXam for example and not restricted to, talc, bentonite, silica, starch ethonium, 18-methoxycoronaridine, carisoprodol, febarbam or maltodextrin among others. ate, meprobamate, metocarbamol, phenprobamate, tibamate, I0085. In another particular embodiment, the delivery sys anticonvulsant agents such as levetiracetam, Stiripentol, phe tem of this invention which contains cosmetic and/or phar nobarbital, methylphenobarbital, , metharbital, maceutical active ingredients and/or adjuvants can be applied , pirimidone, carbamazepine, oXcarbazepine, to the natural or synthetic fibers of textile materials before or benzodiazepines, for example and not restricted to, clon after their manufacture. In this invention textile materials are azepam, cloxazolam, cloraZepate, diazepam, flutoprazepam, understood to be woven fabrics, non-woven fabrics, garments lorazepam, midazolam, nitrazepam, nimetazepam, and medical devices. These textile materials, in direct contact phenazepam, temazepam, tetrazepam or clobazam, among with the body's skin, release the active ingredients incorpo others. rated into the delivery system of this invention either by 0082 In another particular embodiment, the active ingre biodegradation of the of the binding system to the woven dient of the delivery system of this invention is selected from fabric, non-woven fabric or medical device or due to friction the group formed by pharmaceutical active ingredients and/or between these and the body, due to body moisture, the pH of adjuvants. the skin or body temperature. Examples of woven fabrics, US 2013/001 7239 A1 Jan. 17, 2013

non-woven fabrics, garments, medical devices and means for 0090 The cosmetic and/or pharmaceutical compositions immobilization of delivery systems can be found in the prior which comprise the delivery system of this invention can be art (“Impregnating Fabrics With Microcapsules'. HAPPI used in different types of compositions of topical and trans May 1986; Int. J. Pharm. 2002, 242, 55-62, "Biofunctional dermal application which optionally include the cosmetic Textiles and the Skin' Curr. Probl. Dermatol. 2006 v.3. J. and/or pharmaceutically acceptable excipients necessary for Cont. Release 2004, 97,313-320). Means for immobilization the formulation of the desired method of Administration of delivery systems in preferred textile materials are the appli Faulii Trillo C. (1993) en"Tratado de Farmacia Gallénica', cation by means of a foulard, exhaustion bath or spraying. Luzdin 5, S.A. Ediciones, Madrid. The compositions of topi The natural and/or synthetic fibers can be wool, cotton, silk, cal or transdermal application may be presented in any solid, nylon fibers, cellulose, polyamide or polyester among others. liquid or semi-solid formulation, for example and not Among the textile materials the preferred woven fabrics, non restricted to, creams, multiple emulsions, for example and not woven fabrics, garments and medical devices are bandages, restricted to, oil and/or silicone in water emulsions, water-in gauzes, t-shirts, socks, tights, underwear, girdles, gloves, dia oil and/or silicone emulsions, waterfoil/water or water/sili pers, sanitary napkins, dressings, bedspreads, wipes, hydro cone?water type emulsions, and oil/water/oil or siliconefwa gels, adhesive patches, non-adhesive patches, micro-electric ter/silicone type emulsions, anhydrous compositions, patches and/or face masks. aqueous dispersions, oils, milks, balsams, foams, lotions, I0086 According to another aspect, this invention relates gels, cream gels, hydroalcoholic Solutions, hydroglycolic to a cosmetic, pharmaceutical and/or alimentary composition Solutions, hydrogels, liniments, Sera, Soaps, shampoos, con ditioners, serums, polysaccharide films, ointments, mousses, which comprises the delivery system of this invention. pomades, powders, bars, pencils and sprays or aerosols 0087. The delivery system of this invention can be incor (sprays), including leave-on and rinse-off formulations. porated into any form of functional alimentary or enriched These formulations of topical and transdermal application alimentary, or into oral nutricosmetics or cosmetics, and for can be incorporated by techniques known by the people mulated with the usual excipients and adjuvants for oral com skilled in the art into different types of solid accessories, for positions or alimentary Supplements, for example and not example and not restricted to, bandages, gauzes, t-shirts, restricted to, common fatty components, aqueous compo Socks, tights, underwear, girdles, gloves, diapers, sanitary nents, humectants, preservatives, texturizing agents, flavors, napkins, dressings, bedspreads, wipes, adhesive patches, aromas, antioxidants and colorants in the alimentary industry. non-adhesive patches, microelectric patches or face masks, or 0088. The cosmetic, pharmaceutical and/or alimentary can be incorporated into different make-up products Such as compositions which comprise the delivery system of this make-up foundation, for example fluid foundations and com invention can be prepared by the conventional methods pact foundations, make-up removallotions, make-up removal known by the people skilled in the art (“Harry's Cosmeticol milks, under-eye concealers, eye shadows, lipsticks, lip pro ogy'. Eight edition 2000, "Remington. The Science and tectors, lip gloss and powders, among others. The cosmetic or Practice of Pharmacy'. Twentieth edition 2003). The cos dermopharmaceutical compositions of this invention can also metic, pharmaceutical and/or alimentary compositions which be incorporated into products for the treatment and/or care of incorporate the delivery system of this invention can be a final nails and cuticles Such as nail varnishes, nail varnish remover composition, available for application without having to lotions and cuticle remover lotions, among others. carry out any kind of concentration, Solution, dilution, dis 0091. The cosmetic, pharmaceutical and/or alimentary persion, pulverization, spraying procedure or any other simi compositions which comprise the delivery system of this lar procedure known by the person skilled in the art, or an invention can be used in different types of formulations for intermediate composition to which one or several of the pre oral administration, preferably in the form of oral cosmetics vious procedures will be carried out or any other procedure or drugs, for example and not restricted to, capsules, includ known by the person skilled in the art with the aim of obtain ing gelatin capsules, soft capsules, hard capsules, tablets, ing a final composition. including Sugar coated tablets, powders, granules, chewing 0089. The cosmetic, pharmaceutical and/or alimentary gum, Solutions, Suspensions, emulsions, syrups, polysaccha compositions which comprise the delivery system of this ride films, jellies or gelatins, and any otherform known by the invention can be administered by topical or transdermal person skilled in the art. administration, orally, or by any other type of Suitable route, 0092. In another particular embodiment, the compositions for example parenteral, for which the cosmetic and/or phar which comprise the delivery system of this invention can be maceutically acceptable excipients necessary for the formu used for the treatment of textile materials and can be found in lation of the desired method of administration will be washing agents in liquid form, as well as detergents, in the included. In the context of this invention, the term manufacturing of emulsions, rinse aids, rinsing agents, fabric "parenteral' includes nasal, auricular, ophthalmic, rectal, softener, sprays, liquid soaps or gels, or also in Solid form, urethral, vaginal routes, Subcutaneous, intradermal, intravas Such as powder, granules or compact products. In addition, cular injections, such as intravenous, intramuscular, intraocu these compositions contain other components, for example lar, intravitreous, intracorneal, intraspinal, intramedullary, and not restricted to, Surfactants, agents which increase per intracranial, intracervical, intracerebral, intrameningeal, cutaneous absorption, agents for the prior treatment of textile intraarticular, intrahepatic, intrathoracic, intratracheal, materials, agents for the treatment of marks, abrasives, water intrathecal and intraperitoneal, as well as any another similar softeners, fabric softeners, solvents or solubilizing agents, injection or infusion technique. A review of the different agents for the variation of touch and finish, dirt-repelling pharmaceutical forms of administration of the active ingredi agents, antistatic agents, enzymes, agents which aid ironing, ents and excipients necessary for obtaining them can be color and/or colorant brightening agents, shine agents, optical found, for example, in the “Tratado de Farmacia Galénica', clearing agents, graying inhibitors or compounds for the loos C. Fauli i Trillo, 1993, Luzdin 5, S.A. Ediciones, Madrid. ening of dirt, color transfer inhibitors, phobizing and impreg US 2013/001 7239 A1 Jan. 17, 2013 nating agents, Swelling or thickening agents, consistency Example 1 generating agents, silicon agents, agents which increase the percutaneous absorption of microcapsules, whitening agents Preparation of Lipid Nanoparticle Coacervate and textile material bleaching activators, hydrophilization Capsules: Capsules with OctopiroXR agents and/or mixtures thereof. 0093. Another aspect of this invention relates to the use of 0099 Water, Zemea INCI: PROPANEDIOL), phenoxy cosmetic, pharmaceutical and/or alimentary compositions ethanol INCI: PHENOXYETHANOL and sodium hyalur which comprise the delivery system of this invention for the onate INCI: SODIUM HYALURONATE (ingredients A) treatment and/or care of the skin, Scalp, hair and nails. Pref were mixed together in a suitable vessel. Next Centrolex F erably the treatment and/or care of the skin, hair, Scalp and/or INCI: LECITHIN (ingredient B) was slowly added under nails is selected from the group formed by treatment and/or intense helix stirring until complete dispersion. Without ceas prevention of skin aging, healing of the skin and/or scalp. ing the stirring, Inutec SP-1 LINCI: INULIN LAURYL CAR dermatological treatment of skin diseases, treatment and/or BAMATE: WATER (AQUA); ETHYL PYRROLIDONE prevention of cellulitis, tanning of the skin, lightening of the (ingredient C) was added until complete homogeneity was color or bleaching of the skin and treatment and/or prevention achieved. At this point the resulting mixture of ingredients A, of hair loss. B and C was taken to a temperature of 65° C. using a bain 0094. In the context of this invention, the term “aging marie. relates to the changes experienced by the skin with age (chro 0100. In another vessel ingredients D: MYRITOL 318 noaging) or due to exposure to the Sun (photoaging) or to INCI: CAPRYLIC/CAPRIC TRIGLYCERIDE), environmental agents such as Smoke, extreme cli OCTOPIROXR INCI: PIROCTONE OLAMINE), matic conditions of cold or wind, chemical pollutants or CUTINA CPINCI: CETYL PALMITATE), CUTINA CBS pollution, and includes all the external visible changes as well INCI: GLYCERYL. STEARATE: COCOGLYCERIDES; as those noticeable by touch, for example and not restricted CETEARYLALCOHOL: CETYL PALMITATE and DER to, the development of discontinuities on the skin Such as MOFEEL PS INCI: POLYGLYCERYL-3 STEARATE wrinkles, fine lines, furrows, irregularities or roughness, were mixed together and heated to 80°C., occasionally stir increase in the size of pores, loss of elasticity, loss offirmness, ring until achieving homogeneity of the mixture, which was loss of Smoothness, loss of the capacity to recover from the liquid at this temperature. deformation, sagging of the skin Such as sagging cheeks, the 0101 The D mixture was slowly added to the previous appearance of bags under the eyes or the appearance of a mixture of A+B+C under strong mechanical stirring, and double chin among others, changes to the color of the skin once it had been added stirring was continued for 15 minutes Such as marks, reddening, bags under the eyes, appearance of to form a homogenous emulsion. hyperpigmented areas Such as age spots or freckles among 0102 The sample was passed, without cooling, through a others, anomalous differentiation, hyperkeratinization, elas microfluidizer for three cycles at an entrance pressure of 80 tosis, keratosis, hair loss, orange-peel skin, loss of collagen bar and 15000 psion exit, maintaining the operation tempera structure and other histological changes of the stratum cor ture at between 65 and 75° C. neum, of the dermis, epidermis, vascular system (for example the appearance of spider veins or telangiectasias) or of tissues 0103 Solution E was added to the suspension of particles close to the skin, among others. obtained, which was achieved by diluting Quat Soy LDMA 25 INCI: WATER (AQUA); LAURYLDIMONIUM 0095. Another aspect of this invention relates to the use of HYDROXYPROPYL HYDROLYZED SOY PROTEIN) in cosmetic, pharmaceutical and/or alimentary compositions water under light stirring, to finally obtain a homogenous which comprise the delivery system of this invention for the Suspension of encapsulated lipid nanoparticles. treatment of textile materials. In this invention textile mate rials are understood to be woven fabrics, non-woven fabrics, garments and medical devices. Within textile materials the preferred woven fabrics, non-woven fabrics, garments and NGREDIENT (INCI Nomenclature) % IN WEIGHT medical devices are bandages, gauzes, t-shirts, socks, tights, A WATER (AQUA) QSP 100 underwear, girdles, gloves, diapers, sanitary napkins, dress A PROPANEDIOL S.OO ings, bedspreads, wipes, hydrogels, adhesive patches, non A PHENOXYETHANOL 2.00 adhesive patches, microelectric patches and/or face masks. A SODIUM HYALURONATE O.O1 0096. The following specific examples provided herein B LECITHIN S.OO C INULIN LAURYL CARBAMATE: WATER 1.00 serve to illustrate the nature of this invention. These examples (AQUA); ETHYL PYRROLIDONE are included solely for illustrative purposes and should not be D CAPRYLICCAPRIC TRIGLYCERIDE 7.50 construed as limitations on the invention claimed herein. D PIROCTONE OLAMINE 1.00 D CETYL PALMITATE 3.00 D GLYCERYL STEARATE: COCOGLYCERIDES; 3.00 EXAMPLES CETEARYLALCOHOL: CETYL PALMITATE D POLYGLYCERYL-3 STEARATE 1.00 General Methodology E WATER (AQUA): O.20 LAURYLDIMONIUM HYDROXYPROPYL 0097 All the reagents and solvents are of synthesis quality HYDROLYZED SOY PROTEIN and are used without any additional treatment. E WATER (AQUA) 2.00 0098. The high-pressure homogenizations were carried out in a “M110-Y” model microfluidizer by Microfluidics. 0104. The average size of the capsules in suspension The Ultraturrax mixer for the formation of microemulsions is obtained determined by Dynamic Laser Light Scattering was the “D-8” model by Miccra RT. 198 nm. US 2013/001 7239 A1 Jan. 17, 2013

0105. The efficacy of encapsulation was determined by PANEDIOL and phenoxyethanol INCI: PHENOXY passing an aliquot of the Suspension of nanoparticles through ETHANOL (ingredients A) were added in this order. a Sephadex 50 column, centrifuging and Subsequently deter (O112 To the mixture of ingredients A Centrolex FINCI: mining the concentration of the active ingredient OctopiroX LECITHIN (ingredient B) was added drop by drop under INCI: PIROCTONE OLAMINE obtained in the different intense stirring. separated fractions. This determination was carried out by the 0113. In another vessel soybean oil INCI: GLYCINE method supplied by the manufacturer of Octopirox(R) consist SOJA (SOYBEAN) OIL), Lipochroman-6 INCI: DIMETH ing of the spectrophotometric quantification of a piroctone YLMETHOXY CHROMANOL), Cutina CPINCI: CETYL olamine complex with Fe" (Colorimetric determination of PALMITATE, Cutina CRINCI: CETYL RICINOLEATE, Octopirox in ready-to-use cosmetic formulation, operating Cutina CBS INCI: COCOGLYCERIDES and Dermofeel procedure EEH-1200-AA-0036, version 1, 2002, by Clariant PS INCI: POLYGLYCERYL-3 STEARATE (ingredients GMBH). The efficacy of encapsulation was 87.1%. C) were mixed together. The mixture was heated until all the ingredients merged together. Example 2 0114) Next, Retinol S10 INCI: RETINOL (ingredient D) was added to the mixture of ingredients C. Preparation of Lipid Nanoparticle Coacervation 0115 Maintaining phases A+B and C+D at 80°C., C+D Capsules: Capsules with Lipochroman-6 was slowly added to A+B under intense stirring, until an 01.06 Inutec SP-1 INCI: INULIN LAURYL CARBAM emulsion was formed. The heated mixture was stirred vigor ATE was dissolved in water in a suitable vessel. Next, Cen ously with Ultraturrax at 5000 rpm for 30 minutes. Once trolex FINCI: LECITHIN (ingredient A) was slowly added emulsified, the pH was checked and adjusted to 5.50; the and the mixture was heated to 60-70° C. mixture was allowed to cool to room temperature whilst being 0107. In another vessel MYRITOL 318 (INCI: stirred with a turbine. CAPRYLIC/CAPRIC TRIGLYCERIDE), Lipochroman-6 0116. Next, a suspension in water of Quat Soy LDMA 25 INCI: DIMETHYLMETHOXY CHROMANOL), Cutina INCI: LAURYLDIMONIUM HYDROXYPROPYL CPINCI: CETYLPALMITATE, Cutina CRINCI: CETYL HYDROLYZED SOY PROTEIN (ingredients E) was added RICINOLEATE and DERMOFEEL PS INCI: POLYG drop by drop under stirring. Lastly, hyaluronic acid was added LYCERYL-3 STEARATE (ingredients B) were mixed INCI: SODIUM HYALURONATE and stirring was main together. The mixture was heated to 80-90° C. in a water bath tained for 30 minutes until a suitable emulsion was obtained. until totally dissolved. 0108 Next, ingredients B were slowly added to ingredi ents A under intense stirring until achieving a Suitable emul sion and the mixture was left being stirring until it reached NGREDIENT (INCI Nomenclature) % IN WEIGHT room temperature. A WATER (AQUA) QSP 100 0109. In another vessel hyaluronic acid INCI: SODIUM A INULIN LAURYL CARBAMAT S.OO A PROPANEDIOL S.OO HYALURONATE was dissolved in water (ingredient C). A PHENOXYETHANOL 2.60 Once dissolved it was added to the previously prepared emul B LECITHIN S.OO S1O. C GLYCINE SOJA (SOYBEAN) OIL S.OO 0110. Next, Quat Soy LDMA 25 INCI: WATER C DIMETHYLMETHOXY CHROMANOL O.10 C CETYL PALMITATE 3.00 (AQUA); LAURYLDIMONIUM HYDROXYPROPYL C CETYL RICINOLEATE 1.OO HYDROLYZED SOY PROTEIN was added dissolved in C COCOGLYCERIDES 1.OO water under stirring (ingredients D). C POLYGLYCERYL-3 STEARATE 3.00 D RETINOL 2.OO E WATER (AQUA) 2.OO E LAURYLDIMONIUM HYDROXYPROPYL O.20 HYDROLYZED SOY PROTEIN INGREDIENT (INCI Nomenclature) % IN WEIGHT F WATER (AQUA) 1O.OO A WATER (AQUA) QSP 100 F SODIUMHYALURONATE O.O1 A INULINLAURYL CARBAMATE 1.OO A LECITHIN S.OO B CAPRYLIC, CAPRIC TRIGLYCERIDE S.OO B DIMETHYLMETHOXY CHROMANOL 1.OO Example 4 B CETYL PALMITATE 3.00 B CETYL RICINOLEATE 1.OO Preparation of Lipid Nanoparticle Coacervate B POLYGLYCERYL-3 STEARATE 3.00 C SODIUMHYALURONATE O.O1 Capsules: Capsules with Coenzyme Q10 and D LAURYLDIMONIUM HYDROXYPROPYL O.2O Lipochroman-6 HYDROLYZED SOY PROTEIN D WATER (AQUA) 2.OO 0117. In a suitable vessel water, Structure XL INCI: HYDROXYPROPYL STARCH PHOSPHATE), Amigel INCI: SCLEROTIUM GUM), Hyaluronic acid. INCI: SODIUM HYALURONATE), Zemea INCI: PRO Example 3 PANEDIOL and phenoxyethanol INCI: PHENOXY Preparation of Lipid Nanoparticle Coacervate ETHANOL (ingredients A) were added in this order. The Capsules: Capsules with Retinol and Lipochroman-6 mixture was heated in a microwave to 60-65° C. 0118. In another vessel Lipochroman-6 INCI: DIMETH 0111. In a suitable vessel water, Inutec SP-1 INCI: INU YLMETHOXY CHROMANOL), Coenzyme Q10 INCI: LIN LAURYL CARBAMATE), Zemea INCI: PRO UBIQUINONE), Myritol 318 (INCI: CAPRYLIC/CAPRIC US 2013/001 7239 A1 Jan. 17, 2013

TRIGLYCERIDE, Lanette 0 INCI: CETEARYL ALCO Coacervate Capsules with Lipid Nanoparticles and Micro HOL), Emulgade SE DF INCI: CETEARETH-12) and emulsified Vitamin C Arlamol HD INCI: ISOHEXADECANE (ingredients B) I0126. In a suitable vessel water, Amigel INCI: SCLERO were mixed together. The mixture was heated to 80-85°C. TIUM GUM), Zemea INCI: PROPANEDIOL and phe until the ingredients merged together. noxyethanol INCI: PHENOXYETHANOL (ingredients A) 0119 The mixture of ingredients B was added to the mix were mixed together and the mixture was heated in a micro ture of ingredients A, whilst being stirred with a turbine until wave to approximately 50° C. a good emulsion was obtained. 0127. In another vessel, the 0.1% microemulsion of vita 0120 Next, a suspension in water of Quat Soy LDMA 25 min C, soybean oil INCI: GLYCINE SOJA (SOYBEAN) INCI: LAURYLDIMONIUM HYDROXYPROPYL OIL), Lanette 0INCI: CETEARYLALCOHOL), Emulgade HYDROLYZED SOY PROTEIN (ingredients C) was added SEDF INCI: CETEARETH-12) and Arlamol HD INCI: drop by drop under stirring; the stirring was maintained for 10 ISOHEXADECANE (ingredients B) were mixed together. minutes. The mixture was heated until all the ingredients were merged 0121 Finally, the mixture was homogenized under pres together. sure in a microfluidizer for 3 cycles with an entrance pressure I0128. Next, the mixture of ingredients B was added to the of 80 bar and pressure on exit of 15000 psi. Next, the homog mixture of ingredients A, under stirring over about 10 min enized mixture was allowed to cool to room temperature utes. The hot mixture was stirred with Ultraturrax at 5000 rpm whilst being stirred with a turbine. for 30 minutes. Once closely emulsified, the pH was checked and adjusted to 5.50. The mixture was allowed to cool to room temperature whilst being stirred with a turbine. I0129. The hyaluronic acid was added INCI: SODIUM NGREDIENT (INCI Nomenclature) % IN WEIGHT HYALURONATE (ingredient C) to the mixture of A+B A WATER (AQUA) QSP 100 under stirring until it was well homogenized. A HYDROXYPROPYL STARCH PHOSPHATE 1.OO A SCLEROTIUM GUM OSO 0.130 Finally, a suspension in water of Quat Soy LDMA A SODIUMHYALURONATE O.O1 25 INCI: LAURYLDIMONIUM HYDROXYPROPYL A PROPANEDIOL S.OO HYDROLYZED SOY PROTEIN (ingredients D) was added A PHENOXYETHANOL 2.60 drop by drop under stirring, and the mixture was allowed to B DIMETHYLMETHOXY CHROMANOL O.10 B UBIQUINONE S.OO cool whilst being stirred with a turbine. B CAPRYLIC, CAPRIC TRIGLYCERIDE S.OO B CETEARYLALCOHOL 2.OO B CETEARETH-12 3.SO B ISOHEXADECANE 1.OO INGREDIENT (INCI Nomenclature) % IN WEIGHT C WATER (AQUA) 2.OO C LAURYLDIMONIUM HYDROXYPROPYL O.2O A WATER (AQUA) QSP 100 HYDROLYZED SOY PROTEIN A SCLEROTIUM GUM OSO A PROPANEDIOL S.OO A PHENOXYETHANOL 2.6 0122 The average size of the capsules in Suspension B DIETHYLEHEXYL SODIUMSULFOSUCCINATE 1O.OO ISOSTEARIC ACID (15/85), ASCORBIC ACID, obtained determined by Dynamic Laser Light Scattering was WATER (AQUA), ALCOHOL 183 nm. B GLYCINE SOJA (SOYBEAN) OIL 1O.OO B CETEARYLALCOHOL 2.00 Example 5 B CETEARETH-12 3.SO B ISOHEXADECANE 1.00 C SODIUMHYALURONATE O.O1 Preparation of Lipid Nanoparticle Coacervate D WATER (AQUA) 2.00 Capsules: Capsules with Microemulsified Vitamin C D LAURYLDIMONIUM HYDROXYPROPYL O.20 HYDROLYZED SOY PROTEIN 0.1% Vitamin C Microemulsion (0123. In a suitable vessel Ducosate INCI: DIETHYL I0131 The average size of the capsules in suspension HEXYL SODIUMSULFOSUCCINATE) and isostearic acid obtained determined by Dynamic Laser Light Scattering was INCI: ISOSTEARIC ACID were mixed together (phase A). 155 nm. 0.124. In another vessel the vitamin CINCI: ASCORBIC Example 6 ACID was dissolved in water. Once dissolved, the ethanol INCI: ALCOHOL was added (phase B). Preparation of Hydrosoluble Peptide 0.125 Phase B was slowly added to phase A under stirring. Microemulsions for their Subsequent Encapsulation in Coacervate Capsules which Contain Lipid Nanoparticles INGREDIENT (INCI Nomenclature) % IN WEIGHT Example 6-a A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.90 ISOSTEARIC ACID (15/85) B ASCORBIC ACID O.10 Microemulsion of InylineTM B WATER (AQUA) S.OO B ALCOHOL S.OO (0132. In a suitable vessel Ducosate INCI: DIETHYL HEXYL SODIUMSULFOSUCCINATE) and isostearic acid INCI: ISOSTEARIC ACID were mixed together (phaseA). US 2013/001 7239 A1 Jan. 17, 2013

0133. In another vessel the peptide InylineTM INCI: 0.141. In another vessel the peptide Decorinol INCI: ACETYL HEXAPEPTIDE-30 was dissolved in ethanol TRIPEPTIDE-9 CITRULLINE was dissolved in water. INCI: ALCOHOL. Once dissolved, it was added to the Once dissolved, ethanol INCI: ALCOHOL was added water (phase B). (phase B). 0134 Phase B was slowly added to phase A under stirring. 0.142 Phase B was slowly added to phase A under stirring.

INGREDIENT (INCI Nomenclature) % IN WEIGHT INGREDIENT (INCI Nomenclature) % IN WEIGHT A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.955 A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.75 ISOSTEARIC ACID (15/85) ISOSTEARIC ACID (15/85) B ACETYLEHEXAPEPTIDE-30 O.045 B TRIPEPTIDE-9 CITRULLINE O.25 B WATER (AQUA) 2.00 B WATER (AQUA) S.OO B ALCOHOL 8.00 B ALCOHOL S.OO

Example 6-b Example 6-e Microemulsion of Argireline(R) Microemulsion of Decorinyl(R) 0135. In a suitable vessel Ducosate INCI: DIETHYL 0143. In a suitable vessel Ducosate INCI: DIETHYL HEXYL SODIUMSULFOSUCCINATE) and isostearic acid HEXYL SODIUMSULFOSUCCINATE) and isostearic acid INCI: ISOSTEARIC ACID were mixed together (phase A). INCI: ISOSTEARIC ACID were mixed together (phaseA). 0136. In another vessel the peptide Argilerine(R) INCI: 0144. In another vessel the peptide Decorinyl(R) INCI: ACETYL HEXAPEPTIDE-8) was dissolved in water. Once TRIPEPTIDE-10 CITRULLINE was dissolved in water. dissolved, ethanol INCI: ALCOHOL was added (phase B). Once dissolved, ethanol INCI: ALCOHOL was added Phase B was slowly added to phase A under stirring. (phase B). Phase B was slowly added to phase A under stir r1ng.

INGREDIENT (INCI Nomenclature) % IN WEIGHT INGREDIENT (INCI Nomenclature) % IN WEIGHT A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.75 ISOSTEARIC ACID (15/85) A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.75 B ACETYLEHEXAPEPTIDE-8 O.25 ISOSTEARIC ACID (15/85) B WATER (AQUA) S.OO B TRIPEPTIDE-10 CITRULLINE O.25 B ALCOHOL S.OO B WATER (AQUA) S.OO B ALCOHOL S.OO

Example 6-c Example 6-f Microemulsion of Eveseryl R. Microemulsion of SNAP-7 0.137 In a suitable vessel Ducosate INCI: DIETHYL (0145. In a suitable vessel Ducosate INCI: DIETHYL HEXYL SODIUMSULFOSUCCINATE) and isostearic acid HEXYL SODIUMSULFOSUCCINATE) and isostearic acid INCI: ISOSTEARIC ACID were mixed together (phase A). INCI: ISOSTEARIC ACID were mixed together (phaseA). 0.138. In another vessel the peptide Eyeseryl R. INCI: 0146 In another vessel the peptide SNAP-7 INCI: ACETYL TETRAPEPTIDE-5 was dissolved in water. Once ACETYL HEPTAPEPTIDE-4 was dissolved in water. Once dissolved, ethanol INCI: ALCOHOL was added (phase B). dissolved, ethanol INCI: ALCOHOL was added (phase B). 0139 Phase B was slowly added to phase A under stirring. 0147 Phase B was slowly added to phase A under stirring.

INGREDIENT (INCI Nomenclature) % IN WEIGHT INGREDIENT (INCI Nomenclature) % IN WEIGHT A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.50 ISOSTEARIC ACID (15/85) A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.75 B ACETYL TETRAPEPTIDE-5 OSO ISOSTEARIC ACID (15/85) B WATER (AQUA) S.OO B ACETYLEHEPTAPEPTIDE-4 O.25 B ALCOHOL S.OO B WATER (AQUA) S.OO B ALCOHOL S.OO

Example 6-d Example 6-g Microemulsion of Decorinol Microemulsion of SNAP-8 0140. In a suitable vessel Ducosate INCI: DIETHYL 0.148. In a suitable vessel Ducosate INCI: DIETHYL HEXYL SODIUMSULFOSUCCINATE) and isostearic acid HEXYL SODIUMSULFOSUCCINATE) and isostearic acid INCI: ISOSTEARIC ACID were mixed together (phase A). INCI: ISOSTEARIC ACID were mixed together (phaseA). US 2013/001 7239 A1 Jan. 17, 2013

0149. In another vessel the peptide SNAP-7 INCI: -continued ACETYL OCTAPEPTIDE-3 was dissolved in water. Once dissolved, ethanol INCI: ALCOHOL was added (phase B). INGREDIENT (INCI Nomenclature) % IN WEIGHT 0150 Phase B was slowly added to phase A under stirring. C LAURYLDIMONIUM HYDROXYPROPYL O.20 HYDROLYZED SOY PROTEIN

INGREDIENT (INCI Nomenclature) % IN WEIGHT 0157. The average size of the capsules in suspension with A DIETHYLEHEXYL SODIUMSULFOSUCCINATEF 89.75 InylineTM INCI: ACETYL HEXAPEPTIDE-30 obtained ISOSTEARIC ACID (15/85) determined by Dynamic Laser Light Scattering was 102 nm. B ACETYL OCTAPEPTIDE-3 O.25 0158. For the peptide Argilerine(R) INCI: ACETYL B WATER (AQUA) S.OO HEXAPEPTIDE-8), the microemulsion prepared according B ALCOHOL S.OO to example 6-b was used.

Example 7 INGREDIENT (INCI Nomenclature) % IN WEIGHT Preparation of Coacervate Capsules of Lipid A WATER (AQUA) QSP 100 Nanoparticles: Capsules with Microemulsified A SCLEROTIUM GUM OSO Hydrosoluble Peptides A PROPANEDIOL S.OO A PHENOXYETHANOL 2.6 0151. In a suitable vessel water, Amigel INCI: SCLERO A SODIUMHYALURONATE O.O1 TIUM GUM), hyaluronic acid INCI: SODIUM HYALUR B ACETYL HEXAPEPTIDE-8, DIETHYLHEXYL 1O.OO SODIUMSULFOSUCCINATEFISOSTEARIC ONATE), Zemea INCI: PROPANEDIOLand phenoxyetha ACID (15/85), WATER (AQUA), ALCOHOL nol INCI: PHENOXYETHANOL (ingredients A) were B GLYCINE SOJA (SOYBEAN) OIL 1O.OO added in this order, and the mixture was heated in a micro B CETEARYLALCOHOL 2.00 wave to approximately 80°C. B CETEARETH-12 3.SO B ISOHEXADECANE 1.00 0152. In another vessel, the microemulsion of the corre C WATER (AQUA) 2.00 sponding peptide prepared according to example 6, soybean C LAURYLDIMONIUM HYDROXYPROPYL O.20 oil INCI: GLYCINE SOJA (SOYBEAN) OIL), Lanette 0 HYDROLYZED SOY PROTEIN INCI: CETEARYLALCOHOL), Emulgade SEDF (INCI: CETEARETH-12) and Arlamol HD INCI: ISOHEXADE CANE (ingredients B) were added. The mixture was heated 0159. The average size of the capsules in suspension with to 80-85°C. until all the ingredients had merged. Argilerine(R) INCI: ACETYL HEXAPEPTIDE-8) obtained 0153. Next, the mixture of ingredients B was added to the determined by Dynamic Laser Light Scattering was 104 nm. mixture of ingredients A, whilst being stirred with a turbine (0160 For the peptide Eyeseryl R. INCI: ACETYL TET until an emulsion was formed. RAPEPTIDE-5, the microemulsion prepared according to 0154 Next, a suspension in water of Quat Soy LDMA 25 example 6-c was used. INCI: LAURYLDIMONIUM HYDROXYPROPYL HYDROLYZED SOY PROTEIN (ingredients C) was added drop by drop under stirring. 0155 Finally, the mixture was homogenized under pres INGREDIENT (INCI Nomenclature) % IN WEIGHT A WATER (AQUA) QSP 100 sure in a microfluidizer for 3 cycles with an entrance pressure A SCLEROTIUM GUM OSO of 80 bar and an exit pressure of 15000 psi. Next, the homog A PROPANEDIOL S.OO enized mixture was allowed to cool to room temperature A PHENOXYETHANOL 2.6 whilst being stirred with a turbine. A SODIUMHYALURONATE O.O1 B ACETYLTETRAPEPTIDE-5, DIETHYLHEXYL 2O.OO 0156 For the peptide InylineTM INCI: ACETYL SODIUMSULFOSUCCINATEFISOSTEARIC HEXAPEPTIDE-30, the microemulsion prepared according ACID (15/85), WATER (AQUA), ALCOHOL to example 6-a was used. B GLYCINE SOJA (SOYBEAN) OIL 1O.OO B CETEARYLALCOHOL 2.00 B CETEARETH-12 3.SO B ISOHEXADECANE 1.00 C WATER (AQUA) 2.00 INGREDIENT (INCI Nomenclature) % IN WEIGHT C LAURYLDIMONIUM HYDROXYPROPYL O.20 A WATER (AQUA) QSP 100 HYDROLYZED SOY PROTEIN A SCLEROTIUM GUM OSO A PROPANEDIOL S.OO A PHENOXYETHANOL 2.6 0.161 The average size of the capsules in suspension with A SODIUMHYALURONATE O.O1 Eyeseryl(R) INCI: ACETYL TETRAPEPTIDE-5) obtained B ACETYL HEXAPEPTIDE-30, DIETHYLHEXYL 1O.OO SODIUMSULFOSUCCINATEFISOSTEARIC determined by Dynamic Laser Light Scattering was 110 nm. ACID (15/85), WATER (AQUA), ALCOHOL 0162. In the peptide encapsulations, the separation of the B GLYCINE SOJA (SOYBEAN) OIL 1O.OO encapsulated and non-encapsulated active ingredient was car B CETEARYLALCOHOL 2.OO B CETEARETH-12 3.SO ried out by the basket centrifugation technique David W., Fry B ISOHEXADECANE 1.OO et al. Analytical Biochemistry 90: 809-815 (1978). Once C WATER (AQUA) 2.OO both fractions had been separated, the non-encapsulated part was analyzed by HPLC. In no case was peptide presence US 2013/001 7239 A1 Jan. 17, 2013 20 detected in the aqueous phase of the dispersion, therefore, the (0169. In a suitable vessel water and Inutec SP-1 INCI: efficacy of encapsulation is about 100%. INULIN LAURYL CARBAMATE were added in this order. The mixture was stirred until Inutec SP-1 INCI: INULIN Example 8 LAURYL CARBAMATE was correctly dissolved. Next Centrolex FINCI: LECITHIN (ingredients A) was slowly Study of the Comparative Stability of added and the mixture was heated to 60-70° C. Lipochroman-6 in Different Delivery Systems (0170. In another vessel MYRITOL 318 (INCI: (0163 When solutions of Lipochroman-6 INCI: DIM CAPRYLIC/CAPRIC TRIGLYCERIDE), Lipochroman-6 ETHYLMETHOXY CHROMANOL come into contact INCI: DIMETHYLMETHOXY CHROMANOL), Cutina with alcohols they present a change in coloring, changing CPINCI: CETYLPALMITATE, Cutina CRINCI: CETYL from the original Solution’s transparent color to an intense red RICINOLEATE, DERMOFEEL PS INCI: POLYGLYC color over time. ERYL-3 STEARATE (ingredients B) were mixed together. 0164. To demonstrate the greater stabilization abilities of The mixture was heated to 80-90° C. in a water bath until all active ingredients of the lipid nanoparticles capsules, differ the ingredients had completely dissolved. ent delivery systems were prepared containing 0.1% Lipo 0171 The mixture of ingredients B was slowly added to chroman-6 and were subjected to incubation at 40°C. in the the mixtures of ingredients A under light mechanical stirring presence of alcohols for 48 hours. until a suitable emulsion of observable size under an optical microscope was obtained (in the region of 2 um). The final Preparation of Different Delivery Systems Assayed mixture was stirred until the temperature reached 25°C. Example 8-a Example 8-d Standard Preparation of a Suspension of NLC Containing 0.165 Solution of 0.1% Lipochroman-6 in ethanol (stan Lipochroman-6 dard). 0172. The process was exactly the same as in example 2 Example 8-b without including phases C and D. Preparation of a Suspension of Liposomes Example 8-e Containing 1% Lipochroman-6 0166 In a suitable vessel water, vegetable ceramides Suspension of Capsules of Lipid Nanoparticles INCI: LECITHIN, GLYCOLIPIDS), a homogeneous dis Containing Lipochroman-6 persion of Lipochroman-6 INCI: DIMETHYLMETHOXY 0173 They were prepared in the same way as in example CHROMAN in PARSOL MCX INCI: ETHYLHEXYL 2. METHOXYCINNAMATE), a homogeneous mixture of ZEMEA INCI: PROPANEDIOL with phenoxyethanol Stability Assays INCI: PHENOXYETHANOL, EMULMETIK 930 INCI: LECITHIN, LECIFLOR100 IPINCI: Lecithin were added 0.174. The quantitative data from the coloration caused by in this order and under constant mechanical stirring. The the degradation of Lipochroman-6 was obtained by the mixture was heated to 60° C. and INUTEC SP-1 INCI: U/Visible Spectrophotometer technique, measuring the INULIN LAURYL CARBAMATE was added. absorbency of the samples at 295 nm, all diluted at the same 0167. The sample was passed through a microfluidizer concentration. without being cooled for three cycles at an entrance pressure 0.175. The samples for the assay, except the standard, were of 80 bar and 15000 psion exit. prepared according to 1 g solution of suspension of examples 8-a to 8-d in 10 ml of 10% aqueous solution of ethanol. Next, the samples were subjected to incubation at 40° C. for 48 hours. Finally, the absorbency of the samples at 295 nm was INGREDIENT (INCI Nomenclature) % IN WEIGHT measured after carrying out a 1/100 dilution in isopropanol. A WATER (AQUA) QSP 100 (0176 The values obtained are shown in the table below: A LECITHIN, GLYCOLIPIDS 1.OO B DIMETHYLMETHOXY CHROMAN 1.OO B ETHYLEHEXYLMETHOXYCINNAMATE 7.OO C PROPANEDIOL 2O.OO SAMPLE Absorbency ( = 295 nm) C PHENOXYETHANOL 2.60 D LECITEHIN 1.OO 8-a 2.405 E LECITHIN 3.00 8-b 3.204 F INULINLAURYL CARBAMATE O.20 8-d O.291 8-e O.267 Example 8-c 0177. It was observed that the standard solution (sample Preparation of a Suspension of Microparticles 8-a) and the Suspension of liposomes (sample 8-b) saturated Containing 1% Lipochroman-6 the spectrophotometer signal, indicating their degradation in 0168 The process was exactly the same as in example 2 an alcoholic medium. without including phases C and D and carrying out the 0.178 The lipid nanoparticles (sample 8-d) provided a sig homogenization under light stirring. nal intensity lower than the standard solution (sample 8-a). US 2013/001 7239 A1 Jan. 17, 2013

the liposomes (sample 8-b), or the microparticles, but greater 0190. The results obtained were those shown in the table than that of the encapsulated lipid nanoparticles (sample 8-e). below: Therefore, the protection of the active ingredient (Lipochro man-6) from chemical degradation was greater when it was in encapsulated lipid nanoparticles. Retino (%

Example 9 SAMPLE Initial 3 months Study of Comparative Stability of Retinol in 9-a 1.O O.29 Different Delivery Systems 9-c 1.O 0.73 0179 Retinol INCI: DIMETHYLMETHOXY CHRO MANOL is a photolabile active ingredient. To demonstrate the greater stabilization ability of active ingredients of lipid 0191 It could be observed that the lipid nanoparticle cap nanoparticle capsules, different delivery systems containing Sule system would grant retinol more stability than the nano 1% retinol were prepared and were subjected to incubation at particles obtained by complex coacervation, and much more 40° C. for 3 months. The concentration of the active ingredi than the simple retinol emulsion. ent was determined by HPLC. Preparation of the Different Delivery Systems Example 10 Assayed Comparative Percutaneous Absorption Test of Example 9-a Different Delivery Systems Preparation of a 1% Retinol Emulsion 0.192 Percutaneous absorption is a process through which 0180. It is prepared in exactly the same way as that a certain active ingredient passes through the different layers described in example 3 substituting phase C for the following: of skin. This process can be divided into 3 principal stages: 0181 10% Soybean oil INCI: GLYCINE SOJA (SOY penetration, permeation, permeation and resorption. Penetra BEAN) OIL tion is the entrance of the active ingredient into a certain layer 0182 0.1% Lipochroman-6 INCI: DIMETHYL of skin. Permeation is passing through one layer of skin to METHOXY CHROMANOL). another structurally different layer. And resorption is the 0183 Phases E and F of the preparation are also elimi entrance of active ingredient into the vascular system. nated Preparation of the Different Delivery Systems Example 9-b Assayed Preparation of a Suspension of Coacervate Nanocapsules Containing Retinol Example 10-a 0184 The coacervate nanocapsules were prepared in exactly the same way as that described in example 3 Substi Standard tuting phase C for the following: 0185. 10% Soybean oil INCI: GLYCINE SOJA (SOY 0193 2% solution of caffeine in water. BEAN) OIL 0186 0.1% Lipochroman-6 INCI: DIMETHYL Example 10-b METHOXY CHROMANOL). Preparation of a Suspension of Multilamellar Example 9-c Liposomes with Caffeine Preparation of a Suspension of Lipid Nanoparticle 0194 In a suitable vessel water, disodium EDTA INCI: Capsules with Retinol DISODIUM EDTA, Phenonip INCI: PHENOXYETHA 0187. The preparation is described in example 3. NOL, METHYLPARABEN, ETHYLPARABEN, BUTYLPARABEN, PROPYLPARABEN, ISOBUTYLPA Retinol Stability Assay RABEN) and Abiol INCI: IMIDAZOLIDINYLUREA) (in 0188 The emulsion samples (9-a), nanocapsules (9-b) and gredients A) were added in this order, and the mixture was lipid nanoparticle capsules (9-c) were incubated for 3 months mechanically stirred until a homogeneous dispersion was at 40° C. obtained. The pH fell to 3 with a solution of citric acid 0189 For the analysis, 1 g of sample was taken and was (ingredient B). diluted to 10 mL with isopropanol. The dilution mixture was (0195 Without ceasing the stirring, caffeine INCI: CAF subjected to ultrasonication for 5 minutes and was filtered FEINE (ingredient C), CENTROLEX FINCI: LECITHIN using paper to eliminate the wax particles. Finally a 1/25 (ingredient D) were added and stirring was continued for an dilution in isopropanol was carried out, and the simple was extra 30 minutes. Subsequently, the ingredients E: TEAL analyzed by HPLC with a Nucleosil C18 column, using a INCI: CARBOMER and carraghenates INCI: CARRAG methanol/water gradient and measuring the absorbency sig EENANCCHONDRUS CRISPUS) were added, and the pH nal at 326 mm. was adjusted to 6.3 with triethanolamine (ingredient F). US 2013/001 7239 A1 Jan. 17, 2013 22

0200. In another vessel caffeine INCI: CAFFEINE was dissolved in water. Once dissolved, ethanol was added INCI: INGREDIENT (INCI Nomenclature) % IN WEIGHT ALCOHOL (phase B). A WATER (AQUA) QSP 100 0201 Phase B was slowly added to phase A. A DISODIUM EDTA O.15 A PHENOXYETHANOL, METHYLPARABEN, O.38 ETHYLPARABEN, BUTYLPARABEN, PROPYLPARABEN, ISOBUTYLPARABEN INGREDIENT (INCI Nomenclature) % IN WEIGHT A IMIDAZOLIDINYLUREA O.10 B CITRIC ACID, WATER (AQUA) C.S. A DIETHYLEHEXYL SODIUMSULFOSUCCINATE 89.50 C CAFFEINE 2.OO ISOSTEARIC ACID (15/85) D LECITEHIN 4.OO B CAFFEINE OSO E CARBOMER 3.SO B WATER (AQUA) S.OO E CARRAGEENAN (CHONDRUS CRISPUS) 1.OO B ALCOHOL S.OO F TRIETHANOLAMINE C.S.

Example 10-f Example 10-c Preparation of Lipid Nanoparticle Capsules Preparation of a Suspension of Microfluidified Containing Microemulsified Caffeine Liposomes with Caffeine 0202. In a suitable vessel water, Structure XL INCI: 0196. They are prepared in exactly the same way as in the HYDROXYPROPYL STARCH PHOSPHATE) and Amigel previous example incorporating a microfluidification step, INCI: SCLEROTIUMGUM were mixed together. Stir until with 2 cycles at 15000 psi on exit and 80 bar entrance after a homogeneous solution is observed. Next, hyaluronic acid step D and before step E. INCI: SODIUM HYALURONATE was added (ingredients A). Example 10-d 0203. In another vessel the caffeine microemulsion (ex ample 10-e), Lanette 0 INCI: CETEARYL ALCOHOL), Preparation of a Suspension of Mixed Micelles with Emulgade SEDFINCI: CETEARETH-12 and Arlamol HD Caffeine INCI: ISOHEXADECANE were mixed together (ingredi ents B). The mixture was heated until all the ingredients had 0197) In a suitable vessel water adjusted to pH3 with citric merged. acid INCI: CITRIC ACID, caffeine INCI: CAFFEINE), 0204 Mixture B was added to mixture A under continual Dermosoft Octiol INCI: CAPRYLYL GLYCOL), Sensiva stirring, maintaining the two mixtures at 70-80° C. until a SCINCI: ETHYLHEXYLGLYCERIN) and phenoxyetha good emulsion was obtained. Stirring was continued for 15 nol INCI: PHENOXYETHANOL (ingredients A) were minutes. Finally, the mixture was homogenized under pres added in this order, and the mixture was mechanically stirred sure in a microfluidizer for 3 cycles with an entrance pressure at 50° C. until a homogeneous dispersion was obtained. The of 80 bar and an exit pressure of 15000 psi. Next, the homog pH fell to 3 with a solution of citric acid (ingredient B) enized mixture was allowed to cool to room temperature (0198 Without ceasing the stirring, CENTROLEX F whilst being stirred with a turbine. INCI: LECITHIN (ingredient B), and Oramix INCI: CAPRYLYL/CAPRYL GLUCOSIDE, WATER (AQUA) (ingredient E) were added. The final mixture was homog enized under high pressure in a microfluidizer for 2 cycles at INGREDIENT (INCI Nomenclature) % IN WEIGHT a pressure of 15000 psi on exit and 80 bar on entrance. A WATER (AQUA) QSP 100 A HYDROXYPROPYL STARCH PHOSPHATE 1.00 A SCLEROTIUM GUM OSO A SODIUMHYALURONATE O.O1 B DIETHYLEHEXYL SODIUMSULFOSUCCINATE 2O.OO INGREDIENT (INCI Nomenclature) % IN WEIGHT ISOSTEARIC ACID (15/85), CAFFEINE, WATER (AQUA), ALCOHOL A. WATER (AQUA), CITRIC ACID QSP 100 B CETEARYLALCOHOL 2.00 A. CAFFEINE 2.0 B CETEARETH-12 3.SO A. CAPRYLYL GLYCOL O.S B ISOHEXADECANE 1.00 A. ETHYLEHEXYLGLYCERIN O.S A. PHENOXYETHANOL 0.7 B LECITEHIN 3.0 E CAPRYLYLCAPRYL, GLUCOSIDE 3O.O 0205 The average size of the capsules in suspension WATER (AQUA) obtained determined by Dynamic Laser Light Scattering was 99.9 mm. Example 10-g Example 10-e Preparation of Lipid Nanoparticle Capsules Preparation of a 0.5%. Microemulsion with Caffeine Containing Microemulsified Caffeine (0199. In a suitable vessel Ducosate INCI: DIETHYL 0206. In a suitable vessel Centrolex FINCI: LECITHIN HEXYL SODIUMSULFOSUCCINATE) and isostearic acid was added little by little to water until the correct dispersion INCI: ISOSTEARIC ACID were mixed together (phase A). was achieved (ingredient A1). US 2013/001 7239 A1 Jan. 17, 2013

0207. In another vessel, hyaluronic acid INCI: SODIUM 0218. The following table shows the results obtained: HYALURONATE was dissolved in water (ingredients A2). 0208 Next, solution A2 was added to A1 under continual stirring (mixture A). Mixture A was heated in a microwave to 80-850 C. Quantity percutaneously absorped 0209. In another vessel, Lipochroman-6 INCI: DIM SAMPLE (% dosis applied) ETHYLMETHOXY CHROMANOL, caffeine microemul 10-a 2.37 10-b O.99 sion (example 10-e), Cutina CPINCI: CETYL PALMI 10-c. 4.31 TATE, Cutina CBS INCI: COCOGLYCERIDES, Inutec 10-d 1.47 SP1 INCI: INULIN LAURYL CARBAMATE and Dermo 10-e 6.42 feel PS INCI: POLYGLYCERYL-3 STEARATE were 10-g 10.47 mixed together(ingredients B). The mixture was heated until 10-f 18.10 all the ingredients had merged. 0210. Next, mixture B was added to mixture A under con 0219. It could be clearly observed that in the case of the tinual stirring until a good emulsion was obtained. lipid nanoparticle capsules, independently from the type of 0211. The hot mixture obtained (T-75°C.) was homog formulation (10-a, 10-b), there was an important increase in enized under pressure in a microfluidizer for 3 cycles with an cutaneous permeation with regards to the other delivery sys entrance pressure of 80 bar and an exit pressure of 15000 psi. tems assayed. 0212. Once the mixture had been microfluidified, a sus 0220. This result allows the conclusion to be made that the pension in water of Quat Soy LDMA 25 INCI: LAURYLDI lipid nanoparticles capsules constitute a very suitable deliv MONIUM HYDROXYPROPYL HYDROLYZED SOY ery system for incorporation in cosmetic and/or pharmaceu PROTEIN was added drop by drop under stirring (ingredi tical compositions applied to the skin. ents C). 1. A delivery system which comprises lipid nanoparticles 0213. The mixture was allowed to cool to room tempera selected from the group formed by solid lipid nanoparticles ture under stirring. The pH was adjusted to between 5-6 with and nanostructured lipid carriers, containing at least one NaOH. active ingredient and which are polymerically coated with a 0214) Next, Structure XL INCI: HYDROXYPROPYL COacerVate. STARCH PHOSPHATE and Amigel INCI: SCLEROTIUM 2. The delivery system according to claim 1, wherein the GUM were added (ingredients. D), and the mixture was lipids in the lipid nanoparticles can be solid lipids or a mixture stirred until a homogeneous solution was observed. of liquid lipids and solid lipids at room temperature. 0215 Finally, it was allowed to cool whilst being stirred 3. The delivery system according to claim 2, wherein the with a turbine. liquid or semi-liquid lipids are selected from the group formed by vegetable oils, soybean oil, sunflower oil, corn oil, olive oil, palm oil, cotton seed oil, colza oil, peanut oil, coconut oil, castor oil, linseed oil, borage oil, evening prim NGREDIENT (INCI Nomenclature) % IN WEIGHT rose oil, marine oils, fish oils, algae oils, oils derived from A1 WATER (AQUA) QSP 100 petroleum, mineral oil, liquid paraffin, Vaseline, short-chain A1 LECITHIN S.OO fatty alcohols, medium-chain aliphatic branched fatty alco A2 WATER (AQUA) 10.00 A2 SODIUMHYALURONATE O.O1 hols, fatty acid esters with short-chain alcohols, isopropyl B DIETHYLEHEXYL SODIUMSULFOSUCCINATE 2O.OO myristate, isopropyl palmitate, isopropyl Stearate, dibutyl SOSTEARIC ACID (15/85), CAFFEINE, WATER adipate, medium-chain triglycerides, capric and caprylic acid (AQUA), ALCOHOL triglycerides, C-C octanoates; fatty alcohol ethers, dio B DIMETHYLMETHOXY CHROMANO O.O15 B CETYL PALMITATE 1.00 ctyl ether and/or mixtures thereof. B COCOGLYCERIDES 1.00 4. The delivery system according to claim 2, wherein the B INULINLAURYL CARBAMATE 1.00 solid lipids are selected from the group formed by solid trig B POLYGLYCERYL-3 STEARATE 1.00 lycerides, trilaurin, tricaprylin, tripalmitin, tristearin, glyc C WATER (AQUA) 2.00 C LAURYLDIMONIUM HYDROXYPROPYL O.O2 eryl trilaurate, glyceryl trimyristate or trimyristin, glyceryl HYDROLYZED SOY PROTEIN tripalmitate, glyceryl tristearate, glyceryl behenate or tribe D HYDROXYPROPYL STARCH PHOSPHATE 1.00 henin, Solid diglycerides, dipalmitin, distearin, Solid D SCLEROTIUM GUM O.SO monoglycerides, glyceryl monostearate, glyceryl palmito Stearate, glyceryl Stearate citrate, long-chain aliphatic alco 0216. The average size of the capsules in suspension hols, cetyl alcohol, Stearic alcohol, medium and long-chain obtained determined by Dynamic Laser Light Scattering was fatty acids (Co-C), stearic acid, palmitic acid, behenic 137 nm. acid and capric acid, fatty alcohol esters with long and medium-chain fatty acids with polyols (Co-C), fatty alcohol esters of long-chain fatty acids, cetyl palmitate, cet Percutaneous Absorption Test earyl olivate, hydroxyoctacosanyl hydroxy Stearate, Sterols, 0217. In the percutaneous permeation studies, the formu cholesterol, cholesterol esters, cholesteryl hemisuccinate, lation studied was applied to a sample of skin placed in a cholesteryl butyrate, cholesteryl palmitate, fatty amines, Franz diffusion cell. The exposure of the skin to the formu Stearyl amine, waxes, beeswax, shea butter, cocoa butter, lation was maintained for 24 hours. After the 24 hours, the carnauba wax, oZokerite wax, paraffin wax, ceramides, receptor fluid was collected, the skin was washed to eliminate hydrogenated vegetable oils, hydrogenated castor oil, quater the excess preparation and the different layers of the skin nary ammonium derivatives, behenyl trimethyl ammonium were subsequently evaluated by HPLC. chloride, and/or mixtures thereof. US 2013/001 7239 A1 Jan. 17, 2013 24

5. The delivery system according to claim 1, wherein the copolymers, dimethylamino methacrylate, cationic polyacry polymer in the coating of this delivery system is selected from lates and polymethacrylates, polyamine derivatives option the group formed by proteins, polysaccharides, polyesters, ally substituted by derivative polyethylene glycol members, polyacrylates, polycyanoacrylates and/or mixtures thereof. polyamino acids under pH conditions wherein they are cat 6. The delivery system according to claim 5, wherein the ionic, polyethyleneimine, quaternized derivatives of polyvi polymer in the coating of this delivery system is selected from nylpyrrolidone and hydrophilic urethane polymers, as well as the group formed by gelatin, albumin, soy protein, pea pro any mixture of the aforementioned cationic groups. tein, broad bean protein, potato protein, wheat protein, whey protein, B-lactoglobulin, caseinates, wheat Starch, corn 9. The delivery system according to claim 1, wherein the Starch, Zein, alginates, carrageenans, pectins, arabinogalac active ingredient is selected from the group formed by cos tans, gum arabic, Xanthan gum, mesquite gum, tragacanth metic, pharmaceutical and/or alimentary active ingredients gum, galactomannans, guar gum, carob Seed gum, chitosan, and/or adjuvants. agar, poly(L-lysine), dextran Sulfate sodium, carboxymethyl 10. The delivery system according to claim 9, wherein the galactomannan, carboxymethyl cellulose, methyl cellulose, cosmetic and/or alimentary active ingredients and/or adju ethyl cellulose, hydroxypropyl methyl cellulose, cellulose vants are selected from the group formed by Surfactants, nitrate, cellulose acetate butyrate, cellulose acetate phthalate, humectants or Substances which retain moisture, moisturizers hydroxypropyl methylcellulose phthalate, hydroxypropyl or emollients, agents stimulating healing, coadjuvant healing methylcellulose acetate Succinate, polyvinyl acetate phtha agents, agents stimulating re-epithelialization, coadjuvant re late, poly(e-caprolactone), poly(p-dioxanone), poly(Ö-Vale epithelialization agents, agents which synthesize dermal or rolactone), poly(3-hydroxybutyrate), poly(3-hydroxybu epidermal macromolecules, firming and/or redensifying and/ tyrate) and B-hydroxyvalerate copolymers, poly(B- orrestructuring agents, cytokine growth factors, agents which hydroxypropionate), methylacrylic acid copolymers, act on capillary circulation and/or microcirculation, anti-gly dimethylaminoethyl methacrylate copolymers, trimethylam cation agents, free radical scavengers and/or anti-atmo monium ethyl methacrylate copolymers, lactic and glycolic spheric pollution agents, reactive carbonyl species scaven acid polymers and copolymers, lactic and glycolic acid poly gers, 5C-reductase-inhibiting agents, lysyl- and/or prolyl mers and copolymers and polyethylene glycol and mixtures hydroxylase inhibiting agents, defensin synthesis-stimulat thereof. ing agents, bactericidal agents and/or bacteriostatic agents 7. The delivery system according to claim 1, wherein the and/or antimicrobial agents and/or germicidal agents and/or polymer in the polymeric coating of this delivery system is a fungicidal agents and/or fungistatic agents and/or germ-in cationic polymer. hibiting agents, anti-viral agents, antiparasitic agents, anti 8. The delivery system according to claim 7, wherein the histaminic agents, NO-synthase inhibiting agents, descquama cationic polymer is selected from the group formed by cat tion agents or keratolytic agents and/or exfoliating agents, ionic cellulose derivatives, quaternized hydroxyethylcellu comedolytic agents, anti-psoriasis agents, anti-dandruff lose, cationic starches, diallyl ammonium and acrylamide Salt agents, anti-inflammatory agents and/or analgesics, anes copolymers, quaternized vinylpyrrolidone/vinylimidazole thetic agents, anti-wrinkle and/or anti-aging agents, cosmetic polymers, condensation products of polyglycols and amines, and/or absorbent and/or body odor masking deodorants, anti polyduaternium polymers and copolymers, polymers called perspirantagents, perfuming Substances and/or perfumed oils polyduaternium-6, polyduaternium-7. polyduaternium-16, and/or isolated aromatic compounds, anti-oxidizing agents, polyduaternium-10 Merquats, polyduaternium-4 copoly agents inhibiting vascular permeability, hydrolytic epidermal mers, dicocoylethylhydroxyethylammonium, grafting enzymes, whitening or skin depigmenting agents, agents copolymers with a cellulose skeleton and quaternary ammo inhibiting Sweat-degrading enzymes, agents capable offilter nium groups, quaternized collagen polypeptides, laurdimo ing UV rays, agents which stimulate or regulate keratinocyte nium hydroxypropylhydrolyzed collagen, quaternized wheat differentiation, anti-itching agents, agents which stimulate or polypeptides, polyethylenimine, cationic silicone polymers, inhibit the synthesis of melanin, propigmenting agents, self amidomethicone or silicone quaternium-22, adipic acid and tanning agents, agents stimulating the proliferation of mel dimethylamino hydroxypropyl diethylenetriamine copoly anocytes, liquid propellants, vitamins, amino acids, proteins, mers, acrylic acid copolymers with dimethyldiallylammo biopolymers, gelling polymers, skin relaxant agents, agents nium chloride, cationic chitin derivatives, condensation prod capable of reducing or treating bags under eyes, agents for the ucts of cationic dihalogen alkylene, condensation products of treatment and/or care of sensitive skin, astringent agents, dibromobutane with bisdialkylamines, bis-dimethylamino-1, agents regulating sebum production, anti-stretch mark 3-propane, derivatives of cationic guar gum, guar-hydrox agents, lipolytic agents or agents stimulating lipolysis, Veno ypropyltrimonium, quaternary ammonium salt polymers, tonic agents, anti-cellulite agents, calming agents, agents act quaternized polysaccharide polymers of natural derivatives ing on cell metabolism, agents to improve dermal-epidermal Such as azarose, cationic gelatin proteins, cationic gum arabic junction, agents inducing hair growth or hair-loss retardants, proteins, cationic polyamide polymers, cationic polycy body hair growth inhibiting or retardant agents, heat shock anoacrylate polymers, cationic polylactide polymers, cat protein synthesis stimulating agents, muscle relaxants, ionic polyglycolides polymers, cationic polyaniline poly muscle contraction inhibitory agents, agents inhibiting the mers, cationic polypyrrole polymers, cationic aggregation of acetylcholine receptors, anticholinergic polyvinylpyrrolidone polymers, cationic polymers of amino agents, elastase inhibitory agents, matrix metalloproteinase silicone polymers and copolymers, cationic polystyrene inhibitory agents, chelating agents, vegetable extracts, essen polymers, cationic polyvinyl alcohol polymers, cationic tial oils, marine extracts, mineral salts, cell extracts, emulsi polystyrene and maleic acid anhydride copolymers, cationic fying agents, agents stimulating the synthesis of lipids and methyl vinyl ether polymers, cationic epoxy resin polymers, components of the stratum corneum, agents obtained from a cationic polymers of styrene and methyl methacrylate bio-fermentation process and/or mixtures thereof. US 2013/001 7239 A1 Jan. 17, 2013

11. The delivery system according to claim 9, wherein the opioids, antimigraine agents, anticonvulsants, anticholin pharmaceutical active ingredients and/or adjuvants are ergic agents, dopaminergics, antipsychotics, anxiolytics, selected from the group formed by antiacids, agents against hypnotics, sedatives, antidepressants, psychostimulants, anti peptic ulcers and gastroesophageal reflux disease, antispas dementia drugs, parasympathomimetics, drugs used in addic modics, analgesics, anticholinergic drugs, propulsive drugs, tive disorders, anti-vertigo agents, antiparasitic agents, insec antiemetics, antinausea drugs, agents for biliary therapy, ticides, insect repellants, nasal decongestants, mucolytic agents for hepatic therapy, lipotropics, laxatives, antidiarrhe agents, cough Suppressants, ophthalmic active ingredients, tics, intestinal adsorbents, antipropulsives, anti-inflammatory otological active ingredients, antiglaucoma drugs, miotics, drugs, active ingredients against obesity, digestive agents, mydriatics, cycloplegics and/or mixtures thereof. enzymes, hypoglycemic drugs, insulin, vitamins, proteins, 12.-13. (canceled) minerals, anabolic steroids, antithrombotic agents, antifibrin 14. A cosmetic, pharmaceutical and/or alimentary compo olytics, haemostatic agents, antiarrhythmic agents, cardiac sition which comprises the delivery system according to stimulants, cardiac glycosides, vasodilators, antiadrenergic claim 1. agents, antihypertensive drugs, diuretics, potassium-saving 15. The composition according to claim 14, wherein this agents, antihemorrhoidals, antivaricose therapy agents, cap composition is presented in a formulation selected from the illary stabilizing agents, agents which act on the renin-angio group formed by creams, multiple emulsions, anhydrous tensin System, beta-blockers, selective calcium-channel compositions, aqueous dispersions, oils, milks, balsams, blockers, non-selective calcium-channel blockers, ACE foams, lotions, gels, cream gels, hydroalcoholic Solutions, inhibitors, angiotensin II inhibitors, modifying agents of lip hydroglycolic Solutions, hydrogels, liniments, sera, Soaps, ids, antifungals, healing agents, antipruritics, antihistamines, shampoos, conditioners, serums, ointments, mousses, anesthetics, antipsoriatics, chemotherapy drugs, corticoster pomades, powders, bars, pencils, vaporizers, aerosols, cap oids, , disinfectants, anti-acne agents, products for Sules, gelatin capsules, Soft capsules, hard capsules, tablets, gynecological use, oxytocics, anticonceptives, androgen, Sugar coated tablets, granules, chewing gum, Solutions, Sus estrogen, progestagen, gonadotropins, ovulation stimulants, pensions, emulsions, syrups, polysaccharide films, jellies and antiandrogens, products for urological use, antispasmodics, gelatin. drugs used in benign prostatic hypertrophy, hormones, hor 16. The composition according to claim 14, wherein this mone antagonists, antibiotics, tetracyclines, anphenicols, composition is incorporated into a product selected from the beta-lactam antibacterials, penicillin, Sulfonamides, trime group formed by under-eye concealers, make-up foundation, thoprim, macrollides, lincosamides, Streptogramins, antibac make-up removallotions, make-up removal milks, eye shad terial aminoglycosides, antibacterial quinolones, antivirals, ows, lipsticks, lip gloss, lip protectors and powders. immune serum, immunoglobulins, antineoplastic agents, 17. A method of treatment of the skin, scalp, hair and nails immunomodulatory agents, alkylation agents, antimetabo which comprises the administration of the cosmetic, pharma lites, plant alkaloids, cytotoxic antibiotics, immunosuppres ceutical and/or alimentary composition according to claim sive agents, drugs for disorders of the musculoskeletal sys 14. tem, antirheumatics, muscle relaxant agents, agents which 18. Textile material which comprises the cosmetic and/or affect bone structure and mineralization, drugs which act on pharmaceutical composition according to claim 14. the nervous system, general anesthetics, local anesthetics, k k k k k