Microencapsulation and sustained release of biologically active polypeptides

• US 8,129,339 B2
• Filed: 11/06/2008
• Issued: 03/06/2012
• Est. Priority Date: 10/17/2002
• Status: Active Grant

• Current Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Original Assignee: Alkermes Pharma Ireland Limited (Alkermes plc)
• Inventors: Costantino, Henry R., Hotz, Joyce M., Dasch, James R., Riley, M. Gary I., Burke, Paul A., Steitz-Abadi, Susan A., Zale, Stephen E.
• Primary Examiner(s): Cordero Garcia, Marcela M
• Application Number:
  US12/289,857
• Publication Number:
  US 20090281034A1
• Time in Patent Office: 1,216 Days
• Field of Search: None
• US Class Current: 514/6.7
• CPC Class Codes: A61K 38/2278 Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1647 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/5031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
• CPC Class Codes: A61P 3/08 for glucose homeostasis pancreatic hormones A61P5/48
• 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
• CPC Class Codes: A61P 7/12 Antidiuretics, e.g. drugs for diabetes insipidus ADH A61P5/10

Abstract

The invention relates to compositions and methods for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein a biologically active polypeptide, and a corticosteroid to modify the release profile and provide increased bioavailability.

Claims

1. A method for the sustained release in vivo of a biologically active polypeptide, comprising:

administering a sustained release composition that comprises a biocompatible polymer having exendin-4 incorporated therein, and a corticosteroid present in an amount sufficient to modify the release profile of the exendin-4 from the biocompatible polymer and to provide increased bioavailability of the exendin-4, wherein the exendin-4 is released from the sustained release composition for a period of at least about two weeks.

2. The method of claim 1, wherein a weight ratio of the exendin-4 to the corticosteroid is at least 6:

1.

3. The method of claim 2, wherein the corticosteroid is triamcinolone.

4. The method of claim 1, wherein the administering is carried out by injection.

5. The method of claim 1, wherein the exendin-4 is released from the sustained release composition for a period of at least about three weeks.

6. The method of claim 1, wherein the exendin-4 is released from the sustained release composition for a period of at least about four weeks.