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(2) Patent Application Publication (10) Pub. No.: US 2011/0028460 A1 Kisak Et Al

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(2) Patent Application Publication (10) Pub. No.: US 2011/0028460 A1 Kisak Et Al US 201100284.60A1 (19) United States (2) Patent Application Publication (10) Pub. No.: US 2011/0028460 A1 Kisak et al. (43) Pub. Date: Feb. 3, 2011 (54) TOPICAL FORMULATION Publication Classification (75) Inventors: Edward T. Kisak, San Diego, CA (51) Int. Cl. (US); John M. Newsam, La Jolla, A61 K 31/19 (2006.01) CA (US); Dominic King-Smith, A61R 31/195 (2006.01) San Diego, CA (US); Pankaj A61 K 31/40 (2006.01) Karande, Troy, NY (US); Samir A61 K 31/.444 (2006.01) Mitragotri, Goleta, CA (US) A61 K 3.1/541.5 (2006.01) A6IP 29/00 (2006.01) Correspondence Address: FOLEY AND LARDNER LLP (52) U.S. Cl. ...................... 514/226.5: 514/557, 514/567; SUITE 500 514/420; 514/334 3000 K STREET NW WASHINGTON, DC 20007 (US) (57) ABSTRACT (73) Assignee: faubed, Inc. It has been discovered that certain combinations compounds (21) Appl. No.: 12/848,792 are excellent penetration enhancers and, as such, can be incor porated in a topical formulation to facilitate administration of (22) Filed: Aug. 2, 2010 active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin Related U.S. Application Data irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first (63) Continuation-in-part of application No. 12/281,561, compound, and (iii) a second compound, wherein the first filed on Jan. 12, 2009, now Pat. No. 7,795,309, filed as compound and second compound are different, and each is application No. PCT/IB2007/001983 on Mar. 6, 2007. selected from the group consisting of N-lauroyl sarcosine, (60) Provisional application No. 60/778,847, filed on Mar. sodium octyl sulfate, methyl laurate, isopropyl myristate, 6, 2006. oleic acid, glyceryl oleate and sodium lauryl sulfoacetate. US 2011/0028460 A1 Feb. 3, 2011 TOPICAL FORMULATION assisted techniques such as iontophoresis or ultrasound, and bypassing the stratum corneum through microneedle arrays CROSS-REFERENCE TO RELATED or ablation. APPLICATIONS [0008] Molecular or chemical penetration enhancers pro vide an effective and inexpensive means of temporarily [0001] This application is a continuation in part of co reducing skin resistance to the passage of actives and other pending U.S. application Ser. No. 12/281,561, filed on Jan. molecules. Molecular penetration enhancers or ‘MPETM’s’ 12, 2009, which is a national stage of PCT/IB20071001983, can enhance the diffusion of molecules across the skin by, for filed on Mar. 6, 2007, which claims priority to U.S. Provi example, disrupting the lipid bilayers of the stratum corneum. sional Application No. 60/778,847, filed on Mar. 6, 2006, the [0009] Over 300 substances have been identified as entire contents and disclosures of each of which are hereby MPETMs but surprisingly few have been successfully devel incorporated by reference. oped into commercial formulations. Many potent MPETMs are irritating to the cells of the epidermis which can limit both FIELD OF THE INVENTION the choice and concentration of MPETMs suitable for topical formulations. [0002] The present invention relates to a topical formula [0010] Discovery of new MPETM’s to increase skin perme tion of multiplexed molecular penetration enhancers. In a ability is highly desirable and has been an area of high activity particularly preferred embodiment, the present invention over the last 30 years. However, the number of substances relates to a topical formulation of multiplexed molecular pen identified to be penetration enhancers is still small relative to etration enhancers for topical or transdermal administration the more than 25,000,000 substances identified in the CAS of one or more active ingredients such as a pharmaceutical registry (Chemical Abstracts Service, Columbus, Ohio, agent. www.cas.orq). [0011] The number of candidate drugs suitable for topical DESCRIPTION OF THE PRIOR ART and transdermal administration could be significantly increased with improved penetration enhancers. [0003] Topical formulations for application to the skin can [0012] One example of a commercialized formulation for be useful in cosmetic applications, for treating conditions of use intransdermal administration is described in U.S. Pat. No. the upper skin layers and for transdermal administration of 4,575,515 [Sandborn]. Sandborn teaches a formulation that active agents to the local tissue underlying the skin orinto the includes a medicine and dimethyl sulfoxide (DMSO), and blood for systemic distribution. Use of a topical formulation that purportedly allows for rapid and deep penetration of the of for instance, a pharmaceutical agent is advantageous in medicine into the underlying tissue. that it avoids firstpass metabolism, circumvents gastrointes [0013] While the topical formulation taught by Sandborn tinal (“GI”) absorption, can allow delivery of an active ingre represents an advance in the art, there is room for improve dient with a relatively short biological half-life and/or a nar ment. For instance the formulation taught by Sandborn con row therapeutic window and facilitates uniform plasma tains a relatively high concentration of DMSO, which is dosing of the active ingredient, and/or can improve user com known to cause skin irritation. In particular there is a need for pliance. a topical formulation having improved flux of the active [0004] In spite of the advantages, transdermal administra ingredient through the skin as compared to the topical formu tion is usually limited to about a dozen small lipophilic drugs, lation taught by Sandborn. available in transdermal patch format (including scopola mine, fentanyl, estradiol, nitroglycerine, nicotine and test SUMMARY OF THE INVENTION osterone). [0014] It is an object of the present invention to provide a [0005] Skin has evolved to impede the flux of exogenous novel topical formulation. molecules so as to provide a strong barrier to molecular [0015] It is another object of the present invention to pro delivery, particularly agents such as pharmaceutical agents. vide a novel topical formulation for topical or transdermal Transdermal drug administration is difficult since skin is an administration of an active agent. excellent diffusion barrier. [0016] It is another object of the present invention to pro [0006] Structurally, the skin consists of two principle parts: vide a topical formulation capable of providing improved (i) a relatively thin outermost layer (the ‘epidermis’), and (ii) fluxes of therapeutically active agents and other molecules a thicker inner region (the ‘dermis’). The outermost layer of through the skin as compared to the topical formulation the epidermis (the ‘stratum corneum’) consists of flattened taught by Sandborn. dead cells which are filled with keratin. The region between [0017] Accordingly, in one of its aspects, the present inven the flattened dead cells of the stratum corneum is filled with tion provides a topical formulation comprising: (i) at least one lipids which form lamellar phases. The highly impermeable active agent, (ii) a first compound, and (iii) a second com nature of skin is due primarily to the stratum corneum. The pound, wherein the first compound and second compound are viable epidermis underlying the stratum corneum is akin to different, and each is selected from the group of MPETMs other living tissue. The dermis provides the skin’s structural consisting of N-lauroyl sarcosine, sodium octyl sulfate, strength as well as the nerve and vascular networks that sup methyl laurate, isopropyl myristate, oleic acid, glyceryl ole port the epidermis. ate and sodium lauryl sulfoacetate. [0007] Delivering an active agent into orthrough the skin in [0018] In another of its aspects, the present invention pro sufficient concentrations often requires some means for vides a topical formulation for use in topical or transdermal reducing the stratum corneum’s hindrance of penetration. A administration of a substance comprising: (i) at least one number of methods for lowering the stratum corneum’s bar active agent, (ii) a first compound, (iii) a second compound, rier properties have been developed, including electrically and (iv) a therapeutically acceptable carrier that is different US 2011/0028460 A1 Feb. 3, 2011 from the first compound and the second compound, wherein enhancercomprising two or more substances wherein each of the first compound and second compound are different, and the two or more substances is also penetration enhancer. each is selected from the group of MPETM's consisting of [0026] The present inventors have surprisingly and unex N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, pectedly discovered that certain combination of compounds isopropyl myristate, oleic acid, glyceryl oleate and sodium are excellent penetration enhancers and, as such, can be incor lauryl sulfoacetate. porated in a topical formulation to facilitate administration of [0019. In yet another of its aspects, the present invention one or more active ingredients. The increased penetration provides a topical formulation comprising a therapeutically enhancement can also lead to a reduction in the total concen active agent, a therapeutically acceptable carrier and a skin tration of skin irritants in a formulation. penetration enhancer, wherein the skin penetration enhancer [0027] The compounds acting as excellent penetration consists essentially of a mixture of N-lauroyl sarcosine and enhancers are used in combination—i.e., two (or more) com oleic acid. pounds are selected from wherein the first compound and second compound are different, and each is selected from the DETAILED DESCRIPTION OF THE PREFERRED group consisting essentially of N-lauroyl sarcosine, sodium EMBODIMENTS octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, [0020) The present invention provides a topical formula glyceryl oleate and sodium lauryl sulfoacetate. tion that may be used for the topical or transdermal adminis [0028] The preferred combinations of compounds that act tration of at least one active agent. As used throughout this as improved penetration enhancers include the following: specification, the term “transdermal” means in the broadest [0029] the first compound comprises N-lauroyl sar sense through the skin.
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