Transdermal Delivery of Apomorphine Using Microneedles

• US 20110150946A1
• Filed: 08/21/2009
• Published: 06/23/2011
• Est. Priority Date: 08/22/2008
• Status: Abandoned Application

• Current Assignee: Abeer M. Al-Ghananeem
• Original Assignee: Abeer M. Al-Ghananeem
• Inventors: Al-Ghananeem, Abeer M.
• Application Number:
  US13/060,118
• Publication Number:
  US 20110150946A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 9/0021 Intradermal administration, e.g. through microneedle arrays, needleless injectors mechanical aspects A61M
• CPC Class Codes: A61M 2037/0023 Drug applicators using microneedles
• CPC Class Codes: A61M 2037/003 having a lumen
• CPC Class Codes: A61M 2037/0046 Solid microneedles
• CPC Class Codes: A61M 2037/0061 Methods for using microneedles
• CPC Class Codes: A61M 37/0015 by using microneedles
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/30 for treating abuse or dependence

Abstract

The present invention relates generally to methods for transdermal delivery of a therapeutically effective amount of apomorphine using microneedles. The invention also provides methods for treatment of erectile dysfunction and Parkinson'"'"'s disease using apomorphine hydrochloride or any pharmaceutically acceptable salt, and/or apomorphine prodrugs to the microneedle-treated site.

Claims

1. A transdermal drug delivery system comprising a microneedle delivery system wherein the microneedles of the transdermal delivery system are configured to deliver an active pharmaceutical agent transdermally.

2. The transdermal drug delivery system of claim 1 further comprising an active pharmaceutical agent.

3. The transdermal drug delivery system of claim 2, wherein the active pharmaceutical agent is apomorphine.

4. The transdermal drug delivery system of claim 3, wherein the active pharmaceutical agent is a pharmaceutically acceptable salt of apomorphine.

5. The transdermal drug delivery system of claim 4, wherein the pharmaceutically acceptable salt is apomorphine hydrochloride.

6. The transdermal drug delivery system of claim 3, wherein the active pharmaceutical agent is a prodrug of apomorphine.

7. The transdermal drug delivery system of claim 6, wherein the prodrug is water soluble.

8. The transdermal drug delivery system of claim 3, wherein the microneedles are in the form of a microneedle array.

9. The transdermal drug delivery system of claim 3, wherein the microneedle array comprises 15 to 200 microneedles.

10. The transdermal drug delivery system of claim 3, further comprising a dermal drug delivery patch.

11. The transdermal drug delivery system of claim 3, wherein the active pharmaceutical agent provided in a formulation selected from the group consisting of solutions, gels, nanoemulsions, and nanoparticles formulations.

12. The transdermal drug delivery system of claim 3, wherein the active pharmaceutical agent further comprises a hydrophilic polymer, preservative and an antioxidant.

13. A method for administering apomorphine to a subject in need such treatment, comprising administering a therapeutically effective amount of apomorphine pharmaceutical composition, wherein the apomorphine is administered transdermally using an array of microneedles.

14. The method of claim 13, wherein the apomorphine pharmaceutical composition further comprises a hydrophilic polymer, preservative and an antioxidant.

15. A method of treatment for dopaminergic disorders comprising the steps of (i) contacting the skin with an array of microneedles thereby creating a microneedle-treated site in the skin of a subject, and (ii) applying a therapeutically effective amount of apomorphine to the microneedle-treated site.

16. The method of claim 15, wherein the dopaminergic disorder is selected from the group consisting of Parkinson'"'"'s disease, juvenile parkinsonism, schizophrenia, depression, drug addiction, Ramsey-Hunt paralysis syndrome and erectile dysfunction (ED).

17. A method for transdermal delivery of apomorphine, wherein the method comprises the steps of:

(a) creating a microneedle-treated site in the skin of a subject by inserting microneedles into the skin of the subject, followed by;

(b) applying a pharmaceutical composition comprising apomorphine to the microneedle-treated site.

18. The method of claim 17, wherein the microneedle-treated site is created by inserting the microneedles into and removing the microneedles from the skin of the subject prior to application of the apomorphine or any pharmaceutically acceptable salt.

19. The method of claim 17, further comprising the step of abrading a subject'"'"'s skin.

20. The method of claim 17, wherein the skin is abraded prior to administering the pharmaceutical composition.

21. The method of claim 17, wherein the skin is abraded using a device comprising microneedle array.

22. The method of claim 21, wherein the cross-sectional dimension of the microneedles is between about 1 micron and about 200 microns.

23. The method of claim 21, wherein the outer diameter of the microneedle is from about 10 μ

m to about 100 μ

m, and the inner diameter is from about 3 μ

m to about 80 μ

m.

24. The method of claim 21, wherein the length of the microneedles typically is from about 1 μ

m to about 1 mm.

25. The method of claim 21, wherein the microneedle array comprises 15 to 200 microneedles.

26. The method of claim 21, wherein the microneedle array comprises 50 to 100 microneedles.

27. The method of claim 17, wherein the apomorphine is applied to the microneedle-treated site via a topical formulation.

28. The method of claim 17, wherein the topical formulation is selected from the group consisting of a gel, a hydrogel, a topical cream, a salve, and/or an ointment.

29. The method of claim 17, wherein the topical formulation is a gel.

30. The method of claim 17, wherein the pharmaceutical composition comprises about 0.1% to about 90% wt. apomorphine.

31. The method of claim 17, wherein the pharmaceutical composition is a sustained release formulation comprising about 1% to about 30% weight apomorphine.