Arginine heteromers for topical administration
View Patent ↗The invention is directed to a strategy for providing therapeutic or cosmetic benefit to skin by topically applying arginine chemically bound to a second (non-oligo arginine) compound in order to increase transepithelial delivery of arginine through a combination of increased solubility and flux across the skin. The arginine heteromers of the invention can add other complementary or beneficial properties for the skin beyond those that are arginine-related.
1. A heteromer of formula I:
A-R I
wherein A is arginine covalently bonded to a second compound R such that the guanadino group of the arginine remains unreacted,
wherein the covalent bond between A and R is an ether or carbamide linkage,
wherein R is an organic molecule selected from the group consisting of vitamins, fatty acids, and retinoids, and
wherein the heteromer has greater flux across the skin than arginine alone.
2. The heteromer according to claim 1 , wherein R is a vitamin.
3. The heteromer according to claim 2 , wherein R is vitamin C.
4. The heteromer according to claim 2 , wherein R is vitamin E.
5. The heteromer according to claim 2 , wherein R is vitamin D.
6. The heteromer according to claim 1 , wherein R is a fatty acid.
7. The heteromer according to claim 6 , wherein R is palmitic acid or caprylic acid.
8. The heteromer according to claim 1 , wherein R is a retinoid.
9. A composition comprising a cosmetically or dermatologically acceptable carrier; and the heteromer according to claim 1 .
10. The composition according to claim 9 , wherein R is a vitamin.
11. The composition according to claim 10 , wherein R is vitamin C.
12. The composition according to claim 10 , wherein R is vitamin E.
13. The composition according to claim 10 , wherein R is vitamin D.
14. The composition according to claim 9 , wherein R is a fatty acid.
15. The composition according to claim 14 , wherein R is palmitic acid or caprylic acid.
16. The composition according to claim 9 , wherein R is a retinoid.
17. The composition according to claim 9 , further comprising skin-care preparations.
18. The composition according to claim 9 , further comprising bath-preparations.
19. The composition according to claim 9 , further comprising cosmetic preparations.
20. The composition according to claim 9 , further comprising eye-care preparations.
21. The composition according to claim 9 , further comprising lip-care preparations.
22. The composition according to claim 9 , further comprising sunscreen preparations.
23. The composition according to claim 9 , further comprising hair care preparations.
24. The composition according to claim 9 , further comprising an anti-acne preparation.
25. The composition according to claim 9 , further comprising anti-oxidant preparations.
26. The composition according to claim 9 , further comprising anti-psoriasis preparations.
27. The composition according to claim 9 , further comprising corticosteroid preparations.
28. A method for providing a beneficial effect to skin comprising: topically applying a composition comprising the heteromer according to claim 1 .
29. The method according to claim 28 , wherein the beneficial effect is promoting angiogenesis in hair follicles.
30. The method according to claim 28 , wherein the beneficial effect is reducing signs of skin aging.
31. The method according to claim 28 , wherein the beneficial effect is reducing symptoms of acne.
32. The method according to claim 28 , wherein the beneficial effect is reducing damage caused by exposure of the skin to sunlight.
33. The method according to claim 28 , wherein the beneficial effect is reducing the appearance of fine lines and wrinkles in the skin.
34. The method according to claim 28 , wherein the beneficial effect is reducing glandular secretions.
35. The method according to claim 28 , wherein the beneficial effect is providing an anti-oxidant to the skin.
36. The method according to claim 28 , wherein the composition is applied to smooth the texture of skin.
37. The method according to claim 28 , wherein the composition is applied to provide moisturizing and lubricating benefit in the skin.
38. The method according to claim 28 , wherein the second compound is palmitic acid.
39. The method according to claim 38 , wherein the composition is applied to smooth the texture of skin.