Topical systems and methods for treating sexual dysfunction

• US 9,439,926 B2
• Filed: 10/27/2015
• Issued: 09/13/2016
• Est. Priority Date: 03/13/2013
• Status: Active Grant

• Current Assignee: Transdermal Biotechnology, Inc.
• Original Assignee: Transdermal Biotechnology, Inc.
• Inventors: Perricone, Nicholas V.
• Primary Examiner(s): Maewall, Snigdha
• Application Number:
  US14/924,658
• Publication Number:
  US 20160045545A1
• Time in Patent Office: 322 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 38/066 TRH, thyroliberin, thyrotropin releasing hormone
• CPC Class Codes: A61K 38/10 Peptides having 12 to 20 amino acids A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 38/12 Cyclic peptides , e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 38/22 Hormones derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin A61K38/33, e.g. corticotropin A61K38/35
• CPC Class Codes: A61K 38/34 Melanocyte stimulating hormone [MSH], e.g. alpha- or beta-melanotropin
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/1274 Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases, cochleates; Sponge phases

Abstract

The present invention generally relates to compositions and methods for topical or transdermal delivery, and treatment of sexual dysfunction. The compositions can be used in a variety of applications, including treating erectile dysfunction or sexual dysfunction. In some cases, the composition may include nitric oxide and/or peptides. The nitric oxide and/or peptide may be present within a first phase comprising a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present in liposomes, micelles, or other vesicles containing nitric oxide, peptides, or both. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid “stick,” etc., that can be rubbed or sprayed onto the skin, e.g., onto the penis, vulva, or other suitable portion of the skin. The composition can also be applied to a mucosal surface in some instances. Other aspects of the present invention are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.

Claims

1. A method, comprising:

administering, to a subject having or at risk of sexual dysfunction, a composition comprising an effective amount of MSH or an MSH agonist and molecular nitric oxide to treat or prevent the sexual dysfunction, and a carrier comprising phosphatidylcholine containing the molecular nitric oxide, wherein the composition is stable at room temperature.

2. The method of claim 1, wherein the composition is administered to a mucosal surface of the subject.

3. The method of claim 1, wherein the subject is female, and the composition is administered to the vulva of the female subject.

4. The method of claim 1, wherein the subject is male, and the composition is administered to the penis of the male subject.

5. The method of claim 1, wherein the MSH agonist comprises afamelanotide.

6. The method of claim 1, wherein the MSH agonist comprises bremelanotide.

7. The method of claim 1, wherein the MSH agonist comprises Melanotan-II.

8. The method of claim 1, wherein the composition comprises polyenylphosphatidylcholine.

9. The method of claim 1, wherein the composition comprises a liquid crystal structure.

10. The method of claim 1, wherein the composition comprises no more than about 250 ppm of water by weight of the composition.

11. The method of claim 1, wherein the phosphatidylcholine is present at at least about 0.25% by weight of the composition.

12. The method of claim 1, wherein the molecular nitric oxide is present at at least about 0.5% by weight of the composition without nitric oxide.

13. The method of claim 1, wherein the molecular nitric oxide is present within the composition as a gas.

14. The method of claim 1, wherein the molecular nitric oxide is bound by hydrogen bonds or van der Waals forces to the phosphatidylcholine.

15. A method, comprising:

administering, to a subject having or at risk of sexual dysfunction, a composition comprising an effective amount of MSH or an MSH agonist and molecular nitric oxide to treat or prevent the sexual dysfunction, and a carrier comprising phosphatidylcholine containing the molecular nitric oxide, wherein the first phase comprises no more than about 250 ppm of water by weight of the composition.

16. The method of claim 15, wherein the composition is administered to a mucosal surface of the subject.

17. The method of claim 15, wherein the subject is female, and the composition is administered to the vulva of the female subject.

18. The method of claim 15, wherein the subject is male, and the composition is administered to the penis of the male subject.

19. The method of claim 15, wherein the MSH agonist comprises afamelanotide.

20. The method of claim 15, wherein the MSH agonist comprises bremelanotide.

21. The method of claim 15, wherein the MSH agonist comprises Melanotan-II.

22. The method of claim 15, wherein the composition comprises polyenylphosphatidylcholine.

23. The method of claim 15, wherein the composition comprises a liquid crystal structure.

24. The method of claim 15, wherein the composition is stable at room temperature.

25. The method of claim 15, wherein the phosphatidylcholine is present at at least about 0.25% by weight of the composition.

26. The method of claim 15, wherein the molecular nitric oxide is present at at least about 0.5% by weight of the composition without nitric oxide.

27. The method of claim 15, wherein the molecular nitric oxide is present within the composition as a gas.

28. The method of claim 15, wherein the molecular nitric oxide is bound by hydrogen bonds or van der Waals forces to the phosphatidylcholine.

29. A method, comprising:

administering, to a subject having or at risk of sexual dysfunction, a composition comprising an effective amount of TRH and molecular nitric oxide to treat or prevent the sexual dysfunction, and a carrier comprising phosphatidylcholine containing the molecular nitric oxide, wherein the first phase comprises no more than about 250 ppm of water by weight of the composition.

30. The method of claim 29, wherein the composition is administered to a mucosal surface of the subject.

31. The method of claim 29, wherein the subject is female, and the composition is administered to the vulva of the female subject.

32. The method of claim 29, wherein the subject is male, and the composition is administered to the penis of the male subject.

33. The method of claim 29, wherein the composition comprises polyenylphosphatidylcholine.

34. The method of claim 29, wherein the composition comprises a liquid crystal structure.

35. The method of claim 29, wherein the composition is stable at room temperature.

36. The method of claim 29, wherein the phosphatidylcholine is present at at least about 0.25% by weight of the composition.

37. The method of claim 29, wherein the molecular nitric oxide is present at at least about 0.5% by weight of the composition without nitric oxide.

38. The method of claim 29, wherein the molecular nitric oxide is present within the composition as a gas.

39. The method of claim 29, wherein the molecular nitric oxide is bound by hydrogen bonds or van der Waals forces to the phosphatidylcholine.