Microencapsulation and sustained release of biologically active polypeptides

Abstract

This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, 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, a sugar and a salting-out salt.

Description

RELATED APPLICATIONS [0001] This application is a divisional of U.S. application Ser. No. 10 / 688,786, filed on Oct. 17, 2003, which claims the benefit of U.S. Provisional Application No. 60 / 419,388, filed Oct. 17, 2002. The entire teachings of the above applications are incorporated herein by reference.BACKGROUND OF THE INVENTION [0002] Numerous proteins and peptides, collectively referred to herein as polypeptides, exhibit biological activity in vivo, which renders them useful as medicaments in therapy. Many illnesses or conditions which can be treated with a biologically active polypeptide, require administration of a constant or sustained level of medicament to provide the most effective prophylactic and / or therapeutic effects. As such, administration of biologically active polypeptides can require frequent subcutaneous injections, which result in fluctuating levels of medicament and poor patient compliance. [0003] As an alternative, the use of biodegradable materials, such as po...

AI Technical Summary

Benefits of technology

The present invention is about a new way to make medication that releases the active ingredient over time. This is done by adding a combination of sugar and salt to a mixture of a biodegradable polymer and the active ingredient. This results in a more consistent release of the active ingredient over time, which means it can be taken less frequently and still provide the same therapeutic effect. This also reduces the amount of active ingredient needed and makes the medication more tolerable for patients. The method involves dissolving the polymer in a solvent and adding the active ingredient, sugar, and salt. The resulting mixture can be used to make a sustained-release medication for patients with diabetes, obesity, or other metabolic disorders.

Problems solved by technology

As such, administration of biologically active polypeptides can require frequent subcutaneous injections, which result in fluctuating levels of medicament and poor patient compliance.

However, these sustained release devices can exhibit high initial bursts of medicament and minimal release thereafter, resulting in serum drug levels outside the therapeutic window and / or poor bioavailability of the medicament.

In addition, the presence of polymer, physiological temperatures and body response to the sustained release composition can cause the medicament to be altered (e.g., degraded, aggregated) thereby interfering with the desired release profile for the medicament.

Further, methods used to form sustained release compositions can result in loss of activity of the medicament due to the instability of the medicament and the degradative effects of the processing steps.

Degradative effects are particularly problematic when the medicament is a polypeptide.

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