Peptide systems and methods for metabolic conditions

• US 9,724,419 B2
• Filed: 12/04/2013
• Issued: 08/08/2017
• 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:
  US14/096,065
• Publication Number:
  US 20140271934A1
• Time in Patent Office: 1,343 Days
• 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 38/09 Luteinising hormone-releasing hormone [LHRH] , i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
• 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 38/26 Glucagons
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• 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 9/0014 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: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 5/50 for increasing or potentiating the activity of insulin

Abstract

The present invention generally relates to compositions and methods for topical or transdermal delivery, and treatment of metabolic conditions. In some cases, the composition may include nitric oxide and/or peptides such as thyrotropin-releasing hormone (TRH) and/or GnRH (gonadotropin-releasing hormone). 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 structures 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. 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 the skin of a subject having a metabolic condition, a composition comprising an effective amount of thyrotropin-releasing hormone (TRH) and molecular nitric oxide to treat the metabolic condition, and a carrier having a phosphatidylcholine component entrapping the molecular nitric oxide, wherein the composition is stable at room temperature.

2. The method of claim 1, wherein the composition further comprises melanocyte-stimulating hormone (MSH).

3. The method of claim 1, wherein the composition further comprises insulin.

4. The method of claim 1, wherein the composition further comprises exenatide.

5. The method of claim 1, wherein the composition further comprises liraglutide.

6. The method of claim 1, wherein the composition further comprises pramlintide.

7. The method of claim 1, wherein the metabolic condition is metabolic syndrome.

8. The method of claim 1, wherein the metabolic condition is diabetes.

9. The method of claim 1, wherein the metabolic condition is impaired glucose tolerance (IGT).

10. The method of claim 1, wherein the metabolic condition is hyperglycemia.

11. The method of claim 1, wherein the metabolic condition is obesity.

12. The method of claim 1, wherein the molecular nitric oxide is present within the carrier as a gas or bound by hydrogen bonds or van der Waals forces.

13. A method, comprising contacting the skin of a subject having a metabolic condition with a composition comprising:

an emulsion comprising a first phase comprising a thyrotropin-releasing hormone (TRH), molecular nitric oxide, and lecithin, and a second phase comprising an emulsifier, wherein the lecithin is present at least about 0.25% by weight of the composition, and wherein the first phase comprises no more than about 250 ppm of water by weight of the composition.

14. The method of claim 13, wherein the molecular nitric oxide is present within the emulsion as a gas or bound by hydrogen bonds or van der Waals forces to the lecithin.

15. The method of claim 13, wherein at least some of the molecular nitric oxide is present within the first phase bound to phosphatidylcholine.

16. The method of claim 13, wherein the lecithin comprises a phosphatidylcholine, and wherein at least some of the phosphatidylcholine comprises a polyenylphosphatidylcholine.

17. A method, comprising:

administering, to the skin of a subject having a metabolic condition, a composition comprising a first phase comprising an effective amount of thyrotropin-releasing hormone (TRH), molecular nitric oxide, and phosphatidylcholine to treat the metabolic condition, and a second phase comprising an emulsion, wherein the composition comprises no more than about 250 ppm of water by weight of the composition.

18. The method of claim 17, wherein the composition comprises a liquid crystal structure comprising the phosphatidylcholine.

19. The method of claim 18, wherein at least a portion of the liquid crystal structure is multilamellar.

20. The method of claim 17, wherein at least some of the phosphatidylcholine comprises a polyenylphosphatidylcholine.