长春西汀s-PLGA长效缓释微球的体内外评价

In vitro and in vivo evaluation of vinpocetine-loaded sustained-release microspheres with s-PLGA as carrier

目的:本研究以星状聚乳酸羟基乙酸共聚物(star poly D,L-lactide-co-glycolide,s-PLGA)为载体制备长春西汀长效缓释微球,对其体内外性质进行评价。方法:采用开环聚合法制备s-PLGA,以此作为载体材料,采用乳化-溶剂挥发法制备长春西汀s-PLGA长效缓释微球(VIN-MS),并对其包封率、粒径和体内外性质进行了考察。结果:本研究制备的VIN-MS的平均粒径为(18±2)μm,包封率为62.20%,载药量为37.43%。扫描电镜观察结果表明,微球外观圆整、均匀,流动性好,分散性好。体外释放结果表明,VIN-MS具有明显的缓释特性,其突释率为6.96%。体内结果表明,VIN-MS制剂体内周期能维持15 d,与长春西汀普通注射剂相比,VIN-MS的曲线下面积(AUC)和平均滞留时间(MRT)分别是普通注射剂的40倍和38倍。结论:长春西汀s-PLGA长效缓释微球的成功制备将有利于脑血管病的治疗。

Objective ： To investigate the star poly D, L-lactide-co-glycolic acid （ a-PLGA）, as the carriers of vinpocetine-loaded microspheres. Methods： The star polylactic-co-glycolic acid （s-PLGA） was synthesized through ring-opening polymerization reaction. Vinpocetine-loaded sustained-release microspheres with s-PLGA as carriers （VIN-MS） were prepared by solvent evaporation method. The encapsulation efficiency, drug loading, par- ticle size, in vitro and in vivo release were performed. Results： The encapsulation efficiency of the VIN-MS was 62.20% , drug loading was 37.43% , and burst effect was 6.96%. The average size of VIN-MS was （ 18 ±2）μm. In vivo study showed that AUC and MRT of VIN-MS were 40 times and 38 times compared to ordinary VIN injec- tions. Conclusion： Vinpocetine-loaded s-PLGA sustained-release microspheres may be a potential formulation for treating cerebrovascular diseases.