Alpha hydroxy acid sustained release formulation
View Patent ↗An oil-in-water emulsion containing one or more alpha hydroxy acids in which the oil phase of the emulsion contains a high proportion of polar constituents. The emulsion, even at high concentrations of alpha hydroxy acid, is not irritating when applied to the skin.
1. An oil-in-water emulsion comprising a contiguous external aqueous phase and droplets consisting of an internal oil phase suspended in the contiguous external phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar.
2. The emulsion of claim 1 wherein at least 85% w/w of the constituents of the oil phase of the emulsion are polar.
3. The emulsion of claim 1 wherein at least 90% w/w of the constituents of the oil phase of the emulsion are polar.
4. The emulsion of claim 1 wherein at least 95% w/w of the constituents of the oil phase of the emulsion are polar.
5. The emulsion of claim 1 wherein the oil phase of the emulsion is free of constituents that are not polar.
6. The emulsion of claim 1 wherein the emulsifier is selected from the group consisting of cationic emulsifier, non-ionic emulsifier, and weak anionic emulsifier.
7. The emulsion of claim 1 which is free of strong anionic emulsifiers.
8. The emulsion of claim 1 wherein the concentration of the alpha-hydroxy acid is at least 10% w/w.
9. The emulsion of claim 1 wherein the concentration of the alpha-hydroxy acid is at least 12% w/w.
10. The emulsion of claim 1 which is free of mineral oil, petrolatum, and silicone oil.
11. The emulsion of claim 1 which has a relative concentration by weight of polar emollients to non-polar emollients of at least 4:1.
12. The emulsion of claim 1 which has a relative concentration by weight of polar emollients to non-polar emollients of at least 10:1.
13. The emulsion of claim 1 which is free of non-polar emollients.
14. The emulsion of claim 1 wherein the pH of the emulsion is within 1.0 pH units of the dissociation constant (pKa) of the alpha hydroxy acid.
15. The emulsion of claim 14 wherein the pH of the emulsion is within 0.5 pH units of the dissociation constant (pKa) of the alpha hydroxy acid.
16. The emulsion of claim 1 wherein the alpha hydroxy acid is glycolic acid.
17. The emulsion of claim 1 which is free of strontium.
18. A method for treating skin comprising topically applying to the skin of an individual in need thereof an oil-in-water emulsion containing an external aqueous phase and droplets consisting of an oil phase dispersed within the external aqueous phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar.
19. The method of claim 18 wherein the emulsifier is cationic, non-ionic, or weakly anionic.
20. The method of claim 18 wherein the emulsion is free of strong anionic emulsifiers.
21. The method of claim 18 wherein at least 85% w/w of the constituents of the oil phase of the emulsion are polar.
22. The method of claim 18 wherein at least 90% w/w of the constituents of the oil phase of the emulsion are polar.
23. The method of claim 18 wherein at least 95% w/w of the constituents of the oil phase of the emulsion are polar.
24. The method of claim 18 wherein the oil phase of the emulsion is free of constituents that are not polar.
25. The method of claim 18 wherein the concentration of the alpha-hydroxy acid in the emulsion is at least 10% w/w.
26. The method of claim 18 wherein the concentration of the alpha-hydroxy acid in the emulsion is at least 12% w/w.
27. The method of claim 18 wherein the emulsion is free of mineral oil, petrolatum, and silicone oil.
28. The method of claim 18 wherein the emulsion is free of non-polar emollients.
29. The method of claim 18 wherein the pH of the emulsion is within 1.0 pH units of the dissociation constant (pKa) of the alpha hydroxy acid.
30. The method of claim 29 wherein the pH of the emulsion is within 0.5 pH units of the dissociation constant (pKa) of the alpha hydroxy acid.
31. The method of claim 18 wherein the alpha hydroxy acid is glycolic acid.
32. The emulsion of claim 1 wherein each of the constituents of the oil phase has a solubility parameter higher than 7.5.
33. The emulsion of claim 32 wherein each of the constituents of the oil phase has a solubility parameter of 8.0 or higher.
34. The emulsion of claim 33 wherein each of the constituents of the oil phase has a solubility parameter of 8.5 or higher.
35. An oil-in-water emulsion containing an external aqueous phase and an internal phase dispersed within the external aqueous phase, wherein the dispersed phase comprises an oil phase and does not comprise a distinct aqueous area within the oil phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar.
36. An oil-in-water emulsion containing an aqueous phase and an oil phase wherein the aqueous phase is continuous and the oil phase is dispersed within the continuous aqueous phase and wherein the emulsion does not contain a distinct aqueous phase dispersed within the continuous aqueous phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar.
37. An oil-in-water emulsion containing a continuous phase and a dispersed phase within the continuous phase, wherein the continuous phase is an aqueous phase and wherein the dispersed phase consists of an oil phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar.
38. An oil-in-water emulsion comprising an external aqueous phase and an internal oil phase dispersed within the external aqueous phase, which emulsion comprises an alpha-hydroxy acid at a concentration of at least 8.0% w/w, wherein the oil phase of the emulsion comprises a polar emollient and an emulsifier, wherein at least 80% w/w of the constituents of the oil phase of the emulsion, based on the relative amounts of each constituent as used to formulate the emulsion, are polar, and wherein the emulsion is not a multivesicular emulsion.