Journal
JOURNAL OF MICROENCAPSULATION
Volume 36, Issue 8, Pages 747-758Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/02652048.2019.1677795
Keywords
Glucagon-like peptide-1; GLP1; liraglutide; microparticles; long-acting release
Funding
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES) [001]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
- Fundacao de Amparo a Pesquisa do Estado do Rio de Janeiro Carlos Chagas Filho (FAPERJ)
- Programa Nacional de Apoio ao Desenvolvimento da Metrologia, Qualidade e Tecnologia (PRONAMETRO) from the Instituto Nacional de Metrologia, Qualidade e Tecnologia (INMETRO)
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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 mu m. 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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