Method of treating the skin with organic acids in anhydrous microsphere delivery systems

• US 5,962,018 A
• Filed: 04/28/1998
• Issued: 10/05/1999
• Est. Priority Date: 04/28/1998
• Status: Expired due to Term

• Current Assignee: New Avon, LLC (LG Corporation)
• Original Assignee: Avon Products Incorporated
• Inventors: Kaplan, Elinor R., Curtis, Ernest S., Kalafsky, Robert
• Primary Examiner(s): Jarvis, William R. A.
• Application Number:
  US09/069,089
• Time in Patent Office: 525 Days
• Field of Search: 424/450, 514/557, 514/574
• US Class Current: 424/450
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/191 having two or more hydroxy groups, e.g. gluconic acid
• CPC Class Codes: A61K 31/203 Retinoic acids ; Salts thereof
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

Abstract

There is provided a method of treating skin with a therapeutic, water-soluble organic acid. There is also provided an anhydrous composition containing the water-soluble organic acid is encapsulated into hydrophobic microspheres through which the organic acid can elute in the presence of water is applied to the skin. The composition is wet with water immediately prior to, or after the composition is applied to the skin.

Claims

1. A therapeutic composition comprising:

an anhydrous vehicle selected from the group consisting of powder, lotion, solid, cream and gel;

at least one microsphere; and

from about 20 wt %.% to about 30 wt. % of a water-soluble organic acid entrapped within said at least one microsphere

wherein said at least one microsphere is formed of a non-polar copolymer of a carbamate and an acrylate, and wherein the addition of water to the composition facilitates the elution of said water-soluble organic acid from within said at least one microsphere to without said at least one microsphere.

2. The composition of claim 1, wherein said water-soluble organic acid is selected from the group consisting of alpha-hydroxy acids, beta-hydroxy acids, keto-acids, poly-hydroxy carboxylic acids, oxa acids, oxa-diacids and mixtures thereof.

14. The composition of claim 1, wherein the composition is for topical application.

15. The composition of claim 1, wherein said water-soluble organic acid is selected from the group consisting of alpha-hydroxy acids, beta-hydroxy acids, keto-acids, di-alpha-hydroxy acids and poly-hydroxy carboxylic acids, derivatives of retinoic acid, poly-hydroxy carboxylic acids, oxa acids, oxa diacids, and mixtures thereof.

3. A method of treating a skin or hair condition with a therapeutic, water-soluble organic acid, said method comprising:

applying to the skin or hair an anhydrous composition that includes a water-soluble organic acid encapsulated in one or more microspheres through which said organic acid will elute in the presence of water; and

wetting said composition with water immediately prior to, or after applying said composition to the skin or hair,

wherein said skin or hair condition is selected from the group consisting of dry skin, ichthyosis, palmar and plantar hyperkeratoses, dandruff, lichen simplex chronicus, Dariers disease, keratoses, lentigines, age spots, melasmas, blemished skin, acne, psoriasis, eczema, pruritis, inflammatory dermatoses, striae distensae, warts, calluses, ingrown hair, folliculitis, Pseudofolliculitis barbae, photoaging, fine wrinkles, irregular pigmentation, sallowness, loss of skin resilience and loss of elasticity, and

wherein said microsphere is formed of a non-polar copolymer of a carbamate and an acrylate.

4. The method of claim 3, wherein said composition further comprises an anhydrous base material.

5. The method of claim 3, wherein said water-soluble organic acid is selected from the group consisting of alpha-hydroxy acids, beta-hydroxy acids, keto-acids, poly-hydroxy carboxylic acids, oxa acids, oxa di-acids and mixtures thereof in the form of free acids or salts thereof.

6. The method of claim 3, wherein said microspheres are formed of non-polar copolymer of a carbamate and an acrylate.

7. The method of claim 3, wherein said encapsulated water-soluble organic acid is from about 0.1 wt. % to about 70 wt. % of said composition.

8. The method of claim 7, wherein said encapsulated water-soluble organic acid is from about 0.1 wt. % to about 50 wt. % of said composition.

9. The method of claim 3, wherein said composition is in a form selected from the group consisting of dry powders, anhydrous solids, anhydrous lotions, anhydrous creams and anhydrous gels.

10. The method of claim 3, wherein said composition has a pH <

7.

11. The method of claim 10, wherein said composition has a pH <

5.

12. The method of claim 11, wherein said composition has a pH in a range from about 3.5 to about 4.0.

13. The method of claim 3, wherein said composition further comprises at least one additional agent selected from the group consisting of antifungals, vitamins, sunscreens, keratolytic agents, retinoids, antiallergenic agents, depigmenting agents, antiinflammatory agents, anaesthetics, surfactants, moisterizers, exfolients, emulsifiers, antioxidants, insect repellents sunscreen agents, stabilizers, preservatives, antiseptics, emollients, thickeners, lubricants, humectants, chelating agents, fragrances, colorants and skin penetration enhancers.

16. The method of claim 3, wherein said water-soluble organic acid is selected from the group consisting of alpha-hydroxy acids, beta-hydroxy acids, keto-acids, di-alpha-hydroxy acids and poly-hydroxy carboxylic acids, derivatives of retinoic acid, poly-hydroxy carboxylic acids, oxa acids, oxa diacids and mixtures thereof.

17. The method of claim 3, wherein said water-soluble organic acid is a salt of said organic acid, and wherein said salt is derived by neutralization with a base selected from the group consisting of triethanolamine arginine, lysine, potassium hydroxide, sodium hydroxide, lithium hydroxide and ammonium hydroxide.

18. A method for preparing a topical composition useful for delivering a water-soluble organic acid to the skin using an anhydrous vehicle, said method comprising:

encapsulating said water-soluble organic acid into one or more microsphere formed of a non-polar copolymer of a carbamate and an acrylate, and

incorporating said one or more microspheres into an anhydrous vehicle to form an organic acid microsphere composition, and

applying said organic acid microsphere composition to the skin;

wherein the presence of water activates said water-soluble organic acid microsphere composition causing said organic acid to elute from said one or more microspheres.

19. The method of claim 18, wherein said water-soluble organic acid is selected from the group consisting of alpha-hydroxy acids, beta-hydroxy acids, keto-acids, di-alpha-hydroxy acids and poly-hydroxy carboxylic acids, derivatives of retinoic acid, poly-hydroxy carboxylic acids, oxa acids, oxa diacids, and mixtures thereof.

20. The method of claim 18, wherein said water-soluble organic acid is a salt of said water-soluble organic acid, and wherein said salt is derived by neutralization with a base selected from the group consisting of triethanolamine arginine, lysine, potassium hydroxide, sodium hydroxide, lithium hydroxide and ammonium hydroxide.