Laboratory of Pharmaceutical Biotechnology (pbiotech), Faculty of Pharmacy, Federal University of Rio de Janeiro - UFRJ, CCS, Bss24, Rio de Janeiro, Brazil.
Laboratory of Biopolymers and Sensors (LaBioS), Institute of Macromolecules, Federal University of Rio de Janeiro - UFRJ, Rio de Janeiro, Brazil.
J Microencapsul. 2019 Dec;36(8):747-758. doi: 10.1080/02652048.2019.1677795. Epub 2019 Nov 12.
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, release and pharmacologic activity in mice. The resulting microparticles showed size distribution of about 30-50 μm. The kinetic release assays showed a sustained release of the peptides extending up to 30-40 days. 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 pharmacologic activity to the microparticles-loaded liraglutide.
GLP1 受体激动剂在糖尿病、肥胖症及其相关并发症中发挥着重要的调节作用。在此，我们旨在开发负载同源人 GLP1（7-37）或类似物利拉鲁肽的聚合物微球。通过双乳液和溶剂蒸发工艺，使用基于丙交酯（PLA）或丙交酯-乙交酯（PLGA）的 8 种聚合物，制备了载肽微球，并对其粒径分布、形态、释放和在小鼠中的药理活性进行了评价。所得微球的粒径分布约为 30-50μm。动力学释放试验表明，这些肽的释放具有可持续性，可延长至 30-40 天。在瑞士雄性小鼠中的评价表明，单次皮下给予 hGLP1 微球或利拉鲁肽微球后，血糖和体重增加的调节可延长至 25 天。负载 hGLP1 的微球显示出与负载利拉鲁肽的微球相当的药理活性。
