Melanotropin ligands for skin care
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsMinying Cai, Victor J. Hruby, Sean Shelby
Life of this patent
Estimating the term…
Abstract
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.
Claims19
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 the 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:
- 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 the 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 the 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.
A topical composition effective for inducing melanogenesis in epidermal tissue without inducing homologous desensitization of melanocortin-1 receptors, said topical composition comprising a gamma melanocyte stimulation hormone (MSH) analogue, wherein said gamma-MSH analogue is selected from the 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:
- 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.
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 the 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:
- 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-aqueous, non-toxic solvent;
- c. a solute modifier comprising at least one compound selected from the 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. a methylsulfonylmethane;
- e. at least one substance that induces in situ generation of cAMP or cGMP, wherein the substance comprises forskolin;
- f. a skin stabilizer comprising at least one compound selected from the 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;
- g. at least one absorption modifier selected from the group consisting of isopropyl myristate and benzophenone;
- h. at least one fragrance selected from the group consisting of limonene and lemon oil.
Dependencies are inferred from the claim text.