【摘要】 目的制备不同粒径单分散型载艾塞那肽聚乳酸-羟基乙酸共聚物(polylactic-co-glycolic acid,PLGA)微球,考察粒径对包封率及体外释放的影响。方法采用快速膜乳化法结合复乳法制备微球,以10μm SPG膜为例,单因素筛选优化制备条件;扫描电子显微镜观察微球形态,通过测定微球的粒径分布、包封率、体外释放等指标对微球进行评价和比较。结果优化条件下制备了粒径分别为1.917、3.869和18.92μm的单分散型微球,结果显示粒径越小,包封率越低,后期释放越缓慢。结论采用快速膜乳化法可制备出不同粒径的单分散型微球;不同粒径微球的包封率、释放行为差异较大,较大粒径(约20μm)的微球包封率较高,后期稳定持续释放,适合研制成长效缓释微球产品。更多还原

【Abstract】 Objective The aim of this study was to prepare monodisperse exenatide-loaded polylactic-co-glycolic acid(PLGA) microspheres with different size and investigate the size effect on the entrapment efficiency and in vitro release rate of the exenatide-loaded microspheres. Methods The microspheres with different sizes were prepared by premix membrane emulsification. By using single-factor test, the preparation conditions of the microspheres were optimized with the 10 μm SPG membrane. The surface morphology of PLGA microspheres was assessed by scanning electron microscope(SEM). The microspheres were evaluated and compared by particle size distribution, entrapment efficiency(EE) and in vitro release. Results The monodisperse microspheres were prepared respectively with size of 1.917 μm, 3.869 μm, 18.92 μm under the optimized conditions. The results revealed that the microspheres with smaller size obtained lower EE and lower release rate. Conclusions Premix membrane emulsification method could be used to prepare monodisperse microspheres with different sizes. There are apparent discrepancies on the EE and released behavior among the microspheres with different sizes. The microspheres with larger size(about 20 μm) are fitted to be developed into long-term release products, which possessed higher EE and better in vitro release behavior than the others in this study.更多还原