Delivery of polymer conjugates of therapeutic peptides and proteins via coated microprojections

• US 20050106227A1
• Filed: 10/21/2004
• Published: 05/19/2005
• Est. Priority Date: 10/28/2003
• Status: Abandoned Application

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Bentz, Johanna H., Zalipsky, Samuel
• Application Number:
  US10/972,231
• Publication Number:
  US 20050106227A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61B 17/205 Vaccinating by means of needles or other puncturing devices
• CPC Class Codes: A61B 2017/00893 pharmaceutically effective
• CPC Class Codes: A61K 47/56 the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
• 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 2037/0046 Solid microneedles
• CPC Class Codes: A61M 37/0015 by using microneedles

Abstract

An apparatus for transdermally delivering a biologically active agent to a patient comprising a microprojection member having a plurality of microprojections that are adapted to pierce the stratum comeum of the patient, the microprojection member having a biocompatible coating disposed thereon that includes a biologically active agent selected from the group consisting of peptide and protein conjugates.

Claims

1. An apparatus for transdermally delivering a biologically active agent to a patient comprising a microprojection member including a plurality of stratum corneum-piercing microprojections having a biocompatible coating disposed thereon, said biocompatible coating including a biologically active agent selected from the group consisting of peptide and protein conjugates.

2. The apparatus of claim 1, wherein said peptide and protein are conjugated to a polymer selected from the group consisting of polyethyleneglycol, polyvinylpyrrolidone, polyvinylmethylether, polymethyloxazoline, polyethyloxazoline, polyhydroxypropyloxazoline, polyhydroxypropyl-methacrylamide, polymethacrylamide, polydinethyl-acrylamide, polyhydroxypropylmethacrylate, polyhydroxyethylacrylate, hydroxymethylcellulose, hydroxyethylcellulose, polyethyleneglycol, polyaspartamide, copolymers thereof, and polyethyleneoxide-polypropylene oxide.

3. The apparatus of claim 1, wherein each of said microprojections has a length of less than 1000 microns.

4. The apparatus of claim 3, wherein each of said microprojections has a length of less than 300 microns.

5. The apparatus of claim 4, wherein each of said microprojections has a length less than 250 microns.

6. The apparatus of claim 1, wherein said biocompatible coating further comprises a vasoconstrictor.

7. The apparatus of claim 1, wherein said biocompatible coating has a thickness less than approximately 50 microns.

8. The apparatus of claim 1, wherein said biocompatible coating has a thickness less than approximately 25 microns.

9. The apparatus of claim 1, further comprising an applicator having a contacting surface, 1 wherein said microprojection member is releasably mounted on said applicator by a retainer and wherein said applicator, once activated, brings said contacting surface into contact with said microprojection member in such a manner that said microprojection member can strike a stratum comeum of a patient with a power of at least 0.05 joules per cm² of microprojection member in 10 milliseconds or less.

10. A method for transdermally delivering a biologically active agent to a patient, comprising the steps of:

providing a microprojection member having a plurality of microprojections that are adapted to pierce said patient'"'"'s stratum comeum;

coating said microprojection member with a coating formulation having said biologically active agent to form a biocompatible coating, wherein said biologically active agent is selected from the group consisting of peptide and protein conjugates; and

applying said microprojection member to said patient'"'"'s skin, whereby said microprojection members pierce said stratum comeum and deliver said biologically active agent.

11. The method of claim 10, wherein said step of coating said microprojection member comprises immersing said microprojections in said coating formulation.

12. The method of claim 10, wherein said step of coating said microprojection member comprises spraying said coating formulation onto said microprojections.

13. The method of claim 10, further comprising the steps of:

providing an applicator having a contacting surface, wherein said microprojection member is releasably mounted on said applicator by a retainer; and

activating said applicator to bring said contacting surface into contact with said microprojection member in such a manner that said microprojection member strikes said stratum comeum.