DERMAL BARRIER COMPOSITION

• US 20020051797A1
• Filed: 01/04/2000
• Published: 05/02/2002
• Est. Priority Date: 01/04/2000
• Status: Active Grant

• Current Assignee: Skinvisible Pharmaceuticals Incorporated (Skinvisible, Inc.)
• Original Assignee: Skinvisible Pharmaceuticals Incorporated (Skinvisible, Inc.)
• Inventors: JEZIOR, BRUCE
• Granted Patent: US 6,582,683 B2
• Time in Patent Office: Days
• US Class Current: 424/401
• CPC Class Codes: A61K 2800/594 Mixtures of polymers
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 8/8164 Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a carboxyl radical, and containing at least one other carboxyl radical in the molecule, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers, e.g. poly (methyl vinyl ether-co-maleic anhydride)
• CPC Class Codes: A61K 8/8182 Copolymers of vinyl-pyrrolidones. Compositions of derivatives of such polymers
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61Q 17/00 Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
• CPC Class Codes: A61Q 17/005 Antimicrobial preparations
• CPC Class Codes: A61Q 17/02 containing insect repellants
• CPC Class Codes: A61Q 17/04 Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin

Abstract

Disclosed is a dermal barrier composition which contains a hydrophilic polymer emulsion and a hydrophobic polymer emulsion. The dermal barrier composition is moisture activated, and remains inert until the hydrophobic and hydrophilic polymer emulsions contact a suitable substrate such as human skin. The dermal barrier composition is itself an emulsion, and can optionally contain a biocidal agent for antimicrobial and antiviral efficacy. The dermal barrier composition can also contain other active agents such as sunscreens, insect repellents and fungicides. The dermal barrier composition can be applied topically to skin, where it forms a protective or barrier layer against a number of pathogenic and chemical irritants.

Claims

1. A dermal barrier composition for topical application comprising:

(a) a dermal barrier emulsion prepared by mixing a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(b) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(c) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid);

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid).

2. The dermal barrier composition of claim 1 further comprising an active agent.

3. The dermal barrier composition of claim 1 further comprising water.

4. The dermal barrier composition of claim 1 further comprising a thickening agent.

5. The dermal barrier composition of claim 1 further comprising a moisturizing agent.

6. The dermal barrier composition of claim 1 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

40. The method of claim 38 further comprising adding water to the dermal barrier emulsion.

7. A dermal barrier composition for topical application comprising

(a) a dermal barrier emulsion prepared by mixing a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(b) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(c) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid);

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid);

wherein said hydrophilic polymer emulsion and said hydrophobic polymer emulsion are present in a ratio of about 1 to 1.

8. The dermal barrier composition of claim 7 further comprising an active agent.

9. The dermal barrier composition of claim 7 further comprising water.

10. The dermal barrier composition of claim 7 further comprising a thickening agent.

11. The dermal barrier composition of claim 7 further comprising a moisturizing agent.

12. The dermal barrier composition of claim 7 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

14. The dermal barrier composition of claim 13 further comprising an active agent.

15. The dermal barrier composition of claim 13 further comprising water.

16. The dermal barrier composition of claim 13 further comprising a thickening agent.

17. The dermal barrier composition of claim 13 further comprising a moisturizing agent.

18. The dermal barrier composition of claim 13 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

20. The dermal barrier layer of claim 19 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

13. A dermal barrier composition for topical application comprising

(a) a dermal barrier emulsion prepared by mixing a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(b) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(c) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid);

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid);

wherein said hydrophilic polymer emulsion and said hydrophobic polymer emulsion are present in a ratio of about 2.5 to 1.

19. A dermal barrier layer comprising:

(a) a dermal barrier composition comprising a dermal barrier emulsion prepared by mixing a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(b) wherein the dermal barrier emulsion, when applied to dry fritted glass in a thickness of about 0.5 to about 0.85 millimeters and allowed to bond to said glass for a period of 30 seconds, provides a film which remains at least about 80 percent adhered to the fritted glass after treatment with a 5% ammonium hydroxide for a period of 3 hours.

21. A method of making a dermal barrier composition, said method comprising:

(a) preparing a hydrophilic polymer emulsion by mixing;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(b) preparing a hydrophobic polymer emulsion by mixing;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid);

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid);

(c) combining said hydrophilic polymer emulsion and said hydrophobic emulsion with additional components.

22. The method of claim 21 wherein the additional components are one or more of water, a thickening agent, a moisturizing agent, an active agent and combinations thereof.

23. The method of claim 21 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

25. The method of claim 24 further comprising adding an active agent to the dermal barrier emulsion.

26. The method of claim 24 further comprising adding water to the dermal barrier emulsion.

27. The method of claim 24 further comprising adding a thickening agent to the dermal barrier emulsion.

28. The method of claim 24 further comprising adding a moisturizing agent to the dermal barrier emulsion.

29. The method of claim 24 wherein the irritant is a pathogenic irritant.

30. The method of claim 24 wherein the irritant is a chemical irritant.

31. The method of claim 24 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

24. A method for protecting skin tissue against irritants, said method comprising:

(a) washing skin tissue to form cleansed skin tissue; and

(b) contacting said cleansed skin tissue with a dermal barrier emulsion comprising a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(c) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(d) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1 -eicosene); and

(iii) poly (methyl vinyl ether/maleic acid)

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid).

32. A method for protecting skin tissue against excessive moisture loss, said method comprising:

(a) washing skin tissue to form cleansed skin tissue; and

(b) contacting said cleansed skin tissue with a dermal barrier emulsion comprising a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(c) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(d) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid)

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid).

33. The method of claim 32 further comprising adding an active agent to the dermal barrier emulsion.

34. The method of claim 32 further comprising adding water to the dermal barrier emulsion.

35. The method of claim 32 further comprising adding a thickening agent to the dermal barrier emulsion.

36. The method of claim 32 further comprising adding a moisturizing agent to the dermal barrier emulsion.

37. The method of claim 32 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

39. The method of claim 38 wherein:

(a) the hydrophilic polymer emulsion comprises a mixture of;

(i) about 85 to 92 wt-% poly (methyl vinyl ether/maleic acid);

(ii) about 3 to 7 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 4 to 8 wt-% poly (vinyl pyrrolidone/1-hexadecene); and

(b) the hydrophobic polymer emulsion comprises a mixture of;

(i) about 87 to 95 wt-% poly (vinyl pyrrolidone/1-hexadecene);

(ii) about 3 to 8 wt-% poly (vinyl pyrrolidone/1-eicosene); and

(iii) about 2 to 6 wt-% poly (methyl vinyl ether/maleic acid).

41. The method of claim 38 further comprising adding a thickening agent to the dermal barrier emulsion.

42. The method of claim 38 further comprising adding a moisturizing agent to the dermal barrier emulsion.

43. The method of claim 38 wherein the active agent is an antifungal agent.

44. The method of claim 38 wherein the active agent is effective against acne.

45. The method of claim 38 wherein the active agent provides effective sun screen protection.

46. The method of claim 38 wherein the active agent is an insecticide.

48. A barrier layer as set forth in claim 47 above, wherein the layer is from about 5-20 nanometers thick after application and the fenestrations have irregular outlines with spans in the range of 100-1000 nanometers.

49. A barrier layers as set forth in claim 48 above, further including active agents from the class comprising biocides, fungicides, sunscreens and insect repellents.

50. A barrier layer as set forth in claim 49 above, wherein the hydrophilic and hydrophobic polymers are present in ratios of less than 3:

1, and wherein the layer depletes in thickness but remains adherent until the stratum corneum is shed.

51. A barrier layer as set forth in claim 48 above, wherein less than 25% of the layer releases into a 5% bath of ammonium hydroxide after three hours of agitated wash.

52. A barrier layer as set forth in claim 50 above, wherein the hydrophilic and hydrophobic polymers are present in approximately a 1:

1 ratio.

53. A barrier layer as set forth in claim 50 above, wherein the hydrophilic and hydrophobic polymers are present in a ratio of about 2.5:

1.

38. A method of carrying and holding an active agent in proximity to skin tissue, said method comprising:

(a) washing skin tissue to form cleansed skin tissue; and

(b) contacting said cleansed skin tissue with a dermal barrier emulsion comprising a hydrophilic polymer emulsion and a hydrophobic polymer emulsion;

(c) said hydrophilic polymer emulsion comprising a mixture of;

(i) poly (methyl vinyl ether/maleic acid);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (vinyl pyrrolidone/1-hexadecene);

wherein the poly (methyl vinyl ether/maleic acid) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (vinyl pyrrolidone/1-hexadecene);

(d) said hydrophobic polymer emulsion comprising a mixture of;

(i) poly (vinyl pyrrolidone/1-hexadecene);

(ii) poly (vinyl pyrrolidone/1-eicosene); and

(iii) poly (methyl vinyl ether/maleic acid)

wherein the poly (vinyl pyrrolidone/1-hexadecene) is present in an amount greater than either the poly (vinyl pyrrolidone/1-eicosene) or the poly (methyl vinyl ether/maleic acid).

47. A barrier layer for protection for several hours or more of hands and other areas of human skin from reactive and toxic materials that may be encountered in a workplace environment, the barrier layer when in situ comprising:

a formulation including hydrophilic and hydrophobic polymers and establishing a pliant stabilized layer bonded to the stratum corneum of the skin, the layer having a thickness of the order of 10 nanometers and including distributed fenestrations sized to allow excretion from the skin of natural fluids and blocking ingress to the skin of reactive and toxic materials.