Development of an Extended-Release Exenatide Once a Week Depot Formulation

Abstract

Jabar A Faraj, Shaimaa M. Mohammed, Khulood M. Alsaraf, Ihab I. Alkhalifa, Kadum A. Al Shareffi, K. Burton.

Bydureon™, the Exenatide extended-release formulation depot, has been approved in the USA for once weekly treatment for type 2 diabetes mellitus. Exenatide is a synthetic version of exendin-4 with biological properties similar to human glucagon-like peptide-1 (GLP-1) agonist. Evonink Industries at Birmingham - Alabama, USA developed the process based on available reported information to produce Exenatide loaded microparticles that demonstrate a similar in vivo release profile compared to the reference listed drug (RLD). The drug loading, initial burst and other characteristics of the exenatide loaded microparticles are in the range of RLD. Surface characterization by scanning electron microscopy (SEM) of the Evonik produced microparticle visually matches with RLD.