IP Library Granted Patent US 10,828,323
Granted Patent B2
US 10,828,323 · App. 16/251,972 · Granted Nov 10, 2020

Topical compositions and methods of using the same

Inventors: Ryan Doxey (Raleigh, NC); Jian Bao (Cary, NC)
Assignee: Novan, Inc.
A61K33/00A61K8/042A61K8/25A61K8/345A61K8/898A61K9/0014A61K9/06A61K9/10A61K9/107A61K47/02A61K47/10A61K47/12A61K47/14A61K47/32A61K47/38A61K47/44A61K47/52A61K47/59A61Q17/005A61Q19/00A61K2800/22
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Quick Facts
Patent No.
US 10,828,323
App. No.
16/251,972
Granted
Nov 10, 2020
Kind
B2
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.

Claims (31)

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.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2025
From: LNHC, INC.
To: LIGAND PHARMACEUTICALS INCORPORATED
Reel/Frame 071481/0040 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 18, 2024
From: NOVAN, INC.
To: LNHC, INC.
Reel/Frame 066350/0942 →