METHOD OF ENHANCING IONTOPHORETIC DELIVERY OF A PEPTIDE

• US 20090082713A1
• Filed: 09/19/2008
• Published: 03/26/2009
• Est. Priority Date: 09/20/2007
• Status: Abandoned Application

• Current Assignee: Nitric Biotherapeutics, Inc.
• Original Assignee: Nitric Biotherapeutics, Inc.
• Inventors: Friden, Phillip M.
• Application Number:
  US12/234,071
• Publication Number:
  US 20090082713A1
• Time in Patent Office: Days
• US Class Current: 604/21
• CPC Class Codes: A61K 9/0009 involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis microelectromechanical systems A61K9/0097
• CPC Class Codes: A61K 9/0021 Intradermal administration, e.g. through microneedle arrays, needleless injectors mechanical aspects A61M
• CPC Class Codes: A61N 1/303 Constructional details electrodes for external use A61N1/0428
• CPC Class Codes: A61N 1/306 Arrangements where at least part of the apparatus is introduced into the body
• CPC Class Codes: A61N 1/325 for iontophoresis, i.e. transfer of media in ionic state by an electromotoric force into the body electrodes for external use A61N1/0428
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention provides methods for the administration of a peptide to a body surface of the patient comprising treating said body surface by microporation and iontophoretically administering the peptide to the body surface. The present invention also encompasses a method of transdermally administering a peptide to the skin of a patient comprising treating the skin with microporation and iontophoretically administering said peptide to the skin. In one embodiment, the body surface or skin is microporated using one or more microneedles.

Claims

1. A method of transdermally administering a peptide to a patient comprising microporating the skin of the patient with a microneedle while concurrently administering the peptide through the microneedle using iontophoresis.

2. The method of claim 1 wherein the microneedle is hollow.

3. The method of claim 1 wherein the microneedle is porous.

4. The method of claim 1 wherein the skin is microporated with more than one microneedle.

5. The method of claim 4 wherein the skin is microporated with at least about one hundred microneedles.

6. The method of claim 1 wherein the length of the microneedle is less than about 1 mm.

7. The method of claim 1 wherein the microneedle is cylindrical.

8. The method of claim 7 wherein the diameter of the microneedle is about 100 to about 200 μ

m.

9. The method of claim 1 wherein the microneedle is non-cylindrical.

10. The method of claim 9 wherein the cross-sectional length of the microneedle is about 100 to about 200 μ

m.

11. The method of claim 1 wherein said microneedle is attached to or protruding from the surface of a substrate.

12. The method of claim 11 wherein the substrate is made of a flexible material.

13. The method of claim 7 wherein the length of said one or more of microneedles is about 150 to about 900 μ

m.

14. The method of claim 13 wherein the length of the microneedles is about 300 to about 800 μ

m.

15. The method of claim 1 wherein a current density from about 0.1 mA/cm² to about 0.5 mA/cm² is applied.

16. The method of claim 15 wherein the current is applied for about 5 minutes to about 2 hours.

17. The method of claim 1 wherein the peptide is present in a composition comprising a pharmaceutically acceptable excipient.

18. The method of claim 17 wherein the composition further comprises a permeation enhancer.

19. The method of claim 1 wherein the microneedle is made of a material that dissolves upon contact with fluid within the skin.

20. The method of claim 19 wherein the material is a sugar.

21. The method of claim 1 wherein the peptide is a therapeutic protein.

22. The method of claim 1 wherein the peptide has a molecular weight of at least about 1000 Da.

23. The method of claim 1 wherein the peptide has a molecular weight of at least about 3000 Da.

24. A method of transdermally administering a peptide to a patient comprising pretreating the patient'"'"'s skin with microporation using a microneedle followed by administration of said peptide using iontophoresis.

25. The method of claim 24 wherein the microneedle is a solid microneedle.

26. The method of claim 25 wherein the skin is microporated with more than one microneedle.

27. The method of claim 25 wherein the microneedle is made of a material selected from the group consisting of a plastic or a metal.

28. The method of claim 24 wherein the length of the microneedle is about 150 to about 900 um.

29. The method of claim 24 wherein a current density from about 0.1 mA/cm² to about 0.5 mA/cm² is applied.

30. The method of claim 24 wherein the peptide is a therapeutic protein.

31. The method of claim 24 wherein the peptide has a molecular weight of at least about 1000 Da.

32. The method of claim 31 wherein the peptide has a molecular weight of at least about 3000 Da.