Microencapsulation and sustained release of biologically active polypeptides

• US 20090281034A1
• Filed: 11/06/2008
• Published: 11/12/2009
• 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: Steitz-Abadi, Susan A., Burke, Paul A., Costantino, Henry R., Zale, Stephen E., Hotz, Joyce M., Riley, M. Gary I., Dasch, James R.
• Granted Patent: US 8,129,339 B2
• Time in Patent Office: Days
• US Class Current: 514/1.100
• 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 comprising a corticosteroid and a biocompatible polymer having exendin-4 incorporated therein, wherein the exendin-4 is released for a period of at least about two weeks, and wherein the corticosteroid is present in an amount sufficient to modify the release profile of the exendin-4 from the biocompatible polymer and provide increased bioavailability of the exendin-4.

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.