MELANOTROPIN LIGANDS FOR SKIN CARE

摘要

A melanocortin 1 receptor (MC1R) peptide ligand-elastic vesicle complex. The MC1R peptide ligand is modified by coupling the MC1R ligand to a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, elastic vesicles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The MC1R peptide ligand-elastic vesicle complex is prepared as a topical formulation.

主权项

1. A topical composition for transdermal delivery of a gamma melanocyte stimulation hormone (MSH) analogue, said topical composition comprising:
a. the gamma MSH analogue selected from a group consisting of:(SEQ ID NO: 4)H-Lys(hex-5-ynoyl)-Tyr-Val-Nle-Gly-His-DNal(2′)-Arg-DTrp-Asp-Arg-Phe-Gly-NH2;(SEQ ID NO: 5)H-Lys(hex-5-ynoyl)-Tyr-Val-Nle-Gly-His-DNal(2′)-Arg-DPhe-Asp-Arg-Phe-Gly-NH2;(SEQ ID NO: 9)H-Tyr-Val-Nle-Gly-His-DNal(2′)-Arg-DTrp-Asp-Arg-Phe-Gly-NH2;(SEQ ID NO: 11)H-Tyr-Val-Nle-Gly-His-DPhe-Arg-DNal(2′)-Asp-Arg-Phe-Gly-NH2;(SEQ ID NO: 18)H-Tyr-Val-Leu-Gly-His-DPhe-Arg-DNal(2′)-Asp-Arg-Phe-Gly-NH2;and(SEQ ID NO: 19)H-Tyr-Val-Ile-Gly-His-DPhe-Arg-DNal(2′)-Asp-Arg-Phe-Gly-NH2. b. at least one non-toxic solvent; c. a solute modifier comprising at least one compound selected from a group consisting of 3,3′-thiodipropionic acid or an ester or salt thereof, an oxindole alkaloid, a polyphenolic flavonoid, a sugar adduct of a gluconuride, an isoflavone, phosphatidyl serine, phosphatidyl choline, Vitamin D3 and Vitamin K1; d. at least one substance that induces in situ generation of cAMP or cGMP; and e. a skin stabilizer comprising at least one compound selected from a group consisting of an aliphatic carboxylic acid having from about 8 to 32 carbon atoms, an ester of said aliphatic carboxylic acid with an aliphatic alcohol having about 2 to 20 carbon atoms, wherein said ester has a total of about 9 to 36 carbon atoms, and Vitamin D3.