Topical compositions and methods of using the same

Patent metadata

Field	Value
Publication number	US-10828323-B2
Application number	US-201916251972-A
Country	US
Kind code	B2
Filing date	Jan 18, 2019
Priority date	Aug 8, 2013
Publication date	Nov 10, 2020
Grant date	Nov 10, 2020

Abstract

The present invention generally relates to topical compositions and methods of using the same. The topical compositions may comprise a hydrophilic composition and a hydrophobic composition in admixture. The hydrophobic composition may include a nitric oxide-releasing compound such as, for example, a diazeniumdiolate functionalized co-condensed silica particle. In some embodiments, the topical composition may be self-emulsifying. Further described herein are kits comprising a hydrophilic composition and a hydrophobic composition.

First claim

The invention claimed is:

1. A topical composition comprising:
a first composition and a second composition in admixture,
wherein the first composition is a hydrogel having a pH of about 4 to about 5 and the hydrogel has a buffer capacity to maintain the pH of the admixture within about 2 pH units of the hydrogel; wherein the first composition comprises a polymer, polyhydric alcohol, and water;
wherein the second composition comprises a hydrophobic base, an amphiphilic compound, and an active pharmaceutical ingredient comprising a diazeniumdiolate functionalized macromolecule; and
wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration from about 0.01% to about 30% by weight of the second composition.

2. The composition of claim 1 , wherein the hydrogel has a buffer capacity to maintain the pH of the admixture within about 1 pH unit of the hydrogel.

3. The composition of claim 1 , wherein the hydrogel has a buffer capacity to maintain the pH of the admixture within about 0.5 pH units of the hydrogel.

4. The composition of claim 1 , wherein the second composition comprises at least two hydrophobic bases.

5. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration from about 0.01% to about 20% by weight of the second composition.

6. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule comprises a NO-releasing co-condensed silica particle.

7. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule comprises a co-condensed silica network comprising diazeniumdiolated methylaminopropyl trimethoxysilane (MAP3) and tetra methyl orthosilicate (TMOS) and/or diazeniumdiolated methylaminopropyl trimethoxysilane (MAP3) and tetraethyl orthosilicate (TEOS).

8. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration of about 4% by weight of the second composition.

9. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration of about 8% by weight of the second composition.

10. The composition of claim 1 , wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration of about 12% by weight of the second composition.

11. The composition of claim 1 , wherein the first composition comprises a phosphate buffer.

12. The composition of claim 1 , wherein the first composition comprises acetic acid and an acetate.

13. A topical composition comprising:
a first composition and a second composition in admixture,
wherein the first composition is a hydrogel that has a buffer capacity to maintain the pH of the admixture within about 2 pH units of the hydrogel; wherein the first composition comprises a polymer, polyhydric alcohol, and water;
wherein the second composition comprises at least two hydrophobic bases, at least one amphiphilic compound, and an active pharmaceutical ingredient comprising a diazeniumdiolate functionalized macromolecule; and
wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration from about 0.01% to about 30% by weight of the second composition.

14. The composition of claim 13 , wherein the first composition is a hydrogel having a pH of about 4 to about 6.

15. The composition of claim 13 , wherein the hydrogel has a buffer capacity to maintain the pH of the admixture within about 1 pH unit of the hydrogel.

16. The composition of claim 13 , wherein the hydrogel has a buffer capacity to maintain the pH of the admixture within about 0.5 pH units of the hydrogel.

17. The composition of claim 13 , wherein the diazeniumdiolate functionalized macromolecule comprises a co-condensed silica network comprising diazeniumdiolated methylaminopropyl trimethoxysilane (MAP3) and tetra methyl orthosilicate (TMOS) and/or diazeniumdiolated methylaminopropyl trimethoxysilane (MAP3) and tetraethyl orthosilicate (TEOS).

18. A method of treating skin of a subject, the method comprising:
administering an admixture to the skin of the subject, wherein the admixture comprises a first composition and a second composition,
wherein the first composition is a hydrogel having a buffer capacity to maintain the pH of the admixture within about 2 pH units of the hydrogel; wherein the first composition comprises a polymer, polyhydric alcohol, and water;
wherein the second composition comprises at least one hydrophobic base, at least one amphiphilic compound, and an active pharmaceutical ingredient, the active pharmaceutical ingredient comprising a diazeniumdiolate functionalized macromolecule; and
wherein the diazeniumdiolate functionalized macromolecule is present in the second composition at a concentration from about 0.01% to about 30% by weight of the second composition, thereby treating the skin of the subject.

19. The method of claim 18 , wherein the subject has atopic dermatitis.

Assignees

• Novan Inc

Inventors

• Doxey Ryan
• Bao Jian

Classifications

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/0014 Primary

  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 title

• A61K8/06

  Emulsions · CPC title

• A61K8/042

  Gels · CPC title