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Sustained release and pharmacologic evaluation of human glucagon-like peptide-1 and liraglutide from polymeric
Luis Peña Icart1,2, Fernando Gomes de Souza2, Luís Maurício T R Lima1,3
1Laboratory of Pharmaceutical Biotechnology (pbiotech), Faculty of Pharmacy, Federal University of Rio de Janeiro - UFRJ, CCS, Bss24, Rio de Janeiro, Brazil.
Abstract:
The GLP1-receptor agonists exert regulatory key roles in diabetes, obesity and related complications. Here we aimed to develop polymeric microparticles loaded with homologous human GLP1 (7-37) or the analogue liraglutide. Peptide-loaded microparticles were prepared by a double emulsion and solvent evaporation process with a set of eight polymers based on lactide (PLA) or lactide-glycolide (PLGA), and evaluated for particle-size distribution, morphology, in vitro release and pharmacologic activity in mice. The resulting microparticles showed size distribution of about 30-50 μm. The in vitro kinetic release assays showed a sustained release of the peptides extending up to 30-40 days. In vivo evaluation in Swiss male mice revealed a similar extension of glycemic and body weight gain modulation for up to 25 days after a single subcutaneous administration of either hGLP1-microparticles or liraglutide-microparticles. Microparticles-loaded hGLP1 shows equivalent in vivo pharmacologic activity to the microparticles-loaded liraglutide.
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