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WO 2012/059936 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date - i 10 May 2012 (10.05.2012) WO 2012/059936 Al (51) International Patent Classification: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, A61K 9/107 (2006.01) A61K 47/26 (2006.01) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, A61K 47/10 (2006.01) A61K 47/34 (2006.01) ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, A61K 47/20 (2006.01) A61K 47/18 (2006.01) NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, (21) International Application Number: TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, PCT/IN20 11/000730 ZM, ZW. (22) International Filing Date: (84) Designated States (unless otherwise indicated, for every 24 October 201 1 (24.10.201 1) kind of regional protection available): ARIPO (BW, GH, (25) Filing Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, (26) Publication Language: English RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, (30) Priority Data: DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, 3055/MUM/2010 3 November 2010 (03.1 1.2010) IN LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, (72) Inventors; and GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). (71) Applicants : DEVARAJAN, Padma, Venkitachalam [IN/IN]; Department of Pharmaceutical Sciences and Declarations under Rule 4.17 : Technology, Institute of Chemical Technology, N.P. — as to applicant's entitlement to apply for and be granted Marg, Matunga (E), Mumbai 400019, Maharashtra (IN). a patent (Rule 4.1 7(H)) KAPSE, Sonali, Vithal [IN/IN]; N.P. Marg, Matunga — of inventorship (Rule 4.1 7(iv)) (E), Mumbai 400019, Maharashtra (IN). JINDAL, Anil, Brij, Bhushan [IN/IN]; N.P. Marg, Matunga (E), Mum Published: bai 400019, Maharashtra (IN). — with international search report (Art. 21(3)) (81) Designated States (unless otherwise indicated, for every — before the expiration of the time limit for amending the kind of national protection available): AE, AG, AL, AM, claims and to be republished in the event of receipt of AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, amendments (Rule 48.2(h)) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (54) Title: PHARMACEUTICAL COMPOSITIONS FOR COLLOIDAL DRUG DELIVERY (57) Abstract: The present invention relates to preparation of drug loaded heterogeneous nanosystems resulting from mixing of two monophasic phases, the non-aqueous phase comprising of active agent/s, polymers, lipids, surfactants, solubilizer/s and other excipients and the aqueous phase comprising of buffers, isotonic solutions, sweetners, flavors and other excipients.The novel tech- nique enables formation of stable colloidal particles with high drug loading and predictable size at the time of use. The invention © represents a major step in circumventing the technological challenges in the design of colloidal particles which can remain su s pended for at least 4h maintaining an effective average particle size of < 1 π . The unique delivery system makes part of the active agent/s readily bioavailable and part of the agent is present within the polymeric matrix. The invention is applicable to agent/s that contains electrical group, as the particles are formed due to electrostatic interaction. The novel technique avoids use of organic solvent and can reduce energy requirements compared to the conventional preparation methods. The invention is aimed at the overall improvement of therapeutic efficacy, enhance solubility, enhance oral bioavailability and rapid dissolution for in vivo de livery of the BCS class agent/s. The heterogeneous nanosystems /compositions produced according to the invention can be useful in drug delivery, imaging and diagnosis and can be administered by oral and parenteral route. FIELD OF INVENTION The present invention discloses pharmaceutical compositions comprising two monophasic liquids which on mixing form drug loaded heterogeneous nanosystems of average size < 1 η. The heterogeneous nanosystems comprises of nanoparticles, micelles, nano-drug particles crystalline or amorphous. The said monophasic liquid compositions comprise of at least one active agent and pharmaceutically acceptable excipients. The particulate compositions produced according to the invention can be useful in drug delivery, imaging and diagnosis and can be administered by oral and parenteral routes. SUMMARY OF THE INVENTION The present invention discloses pharmaceutical compositions an aqueous liquid composition and a non aqueous liquid composition which on mixing form drug loaded heterogeneous nanosystems of average size < 1µπι. The aqueous liquid composition comprises polymer/s biodegradable and non-biodegradable, surfactants include cationic, anionic and nonionic, surface modifying agents including hydrophilic polymers, carbohydrate, proteins and receptor specific ligands, pH modulators includes buffers, acid and bases, stabilizers include antioxidants, absorption enhancers, targeting ligands. The non-aqueous liquid composition comprises surfactant/s cationic, anionic and nonionic, polymer/s biodegradable and non-biodegradable, ipid s fatty acids and glycerol esters of fatty acids and at least one non-aqueous solvent. Active agent is dissolved in either aqueous composition or non-aqueous composition. The drug loaded heterogeneous nanosystems of said inventions are generated by mixing the aqueous and non-aqueous compositions in a predetermined ratio. OBJECTIVE OF THE INVENTION The objective of the invention is to provide pharmaceutical compositions comprising two monophasic liquids which on mixing form drug loaded heterogeneous nanosystems of average size < 1µ that have improved bioavailability. The another objective of the invention is to provide pharmaceutical compositions comprising two monophasic Mquids which on mixing form drug loaded heterogeneous nanosystems of average size < 1µ η that have f Oved efficacy. Ρ the another objective of the invention is to provide pharmaceutical composition comprising two a ophasic liquids comprising of active agent/s and pharmaceutically acceptable excipients which on mixing form drug loaded heterogeneous nanosystems of size < 1µπι that is simple to prepare and scale up. Yet the another objective of the invention is to provide pharmaceutical composition comprising two monophasic liquids comprising of drug s and pharmaceutically acceptable excipients which on mixing form drug loaded heterogeneous nanosystems of size < 1µπ that may be targeting to specific body site. BACKGROUND AND PRIOR ART Drug loaded heterogeneous nanosystems including polymeric micro/nanoparticles, solid lipid nanoparticles, polymer-lipid hybrid particles, micelles etc. have been extensively investigated as potential carriers for drug delivery in recent years for a wide range of applications particularly for chemotherapeutic agents in oral and parenteral delivery. For improved efficacy and enhanced effectiveness of such carriers for in vivo delivery in therapy the size, shape, surface morphology along with high drug loading are important, since the latter decreases the manufacturing cost thereby increasing patient compliance and reducing the administration dose with reduced undesirable side effects. Conventional methods for the preparation of nanoparticles include nanoprecipitation, emulsion solvent evaporation and emulsion solvent diffusion. Nanoparticles generated by these methods are isolated by centrifugation, filtered and dried preferentially by freeze drying to obtain dried particulate carriers which are reconstituted with aqueous medium. Problems encountered by these methods are undesirable particle heterogeneity as the matrix material and the drug molecules tend to self-aggregate during nanoprecipitation. Also problems associated with maintaining the integrity of the liquid suspension for a prolonged time period, despite addition of surface active agents to stabilize the suspension little aggregation is often observed upon storage. Improvement in stability represents an important issue in the development of these drug carriers. Freeze-drying 4 is one of the most suitable methods to stabilize and facilitate the handling of colloidal systems. Increase in particle size after freeze drying is another significant problem. Inherent technological problems associated with production scale-up and commercialization of such carriers/systems by conventional methods limits their production in large quantities. In an attempt to bypass the scale up challenges in the design of drug loaded particulate carriers, a simple yet unique approach for the preparation of heterogeneous nanosystems by in-situ nanoprecipitation method has been developed. The developed methodology provides drug loaded heterogeneous nanosystems with good batch-to-batch reproducibility. The invention provides a simple, one-step strategy for preparation of heterogeneous nanosystems with >50% entrapment efficiency. Among the methods reported for preparation of particulate carriers, nanoprecipitation is a single step, instantaneous method based on interfacial turbulence without application of external energy for reproducible formation of nanoparticles below 1 micron with low polydispersity index and high yields of hydrophobic drugs. The present invention discloses pharmaceutical
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