伏立康唑PLGA纳米微粒的制备及其形态和释放特点分析

Preparation,Morpha and In Vitro Release of Poly(D,L-Lactic-co-glycolic Acid)Nanoparticles Containing Voriconazole

目的制备伏立康唑PLGA纳米微粒,并分析其形态及释放特点。方法采用乳化-溶剂挥发法制备伏立康唑PLGA纳米微粒,用激光粒径分析仪及扫描电镜分别进行分散性和形态学分析,经HPLC分析其载药量及释放特点。结果经激光粒径分析,样品粒径峰值为(126±20)nm,分布指数为1.5。电镜观察颗粒分布均匀,表面光滑。HPLC分析载药量为(1.9±0.6)%,包封率约为12%,24h内存在突释,第2天到第8天缓慢释放。结论已成功制备了伏立康唑PLGA纳米微粒,能实现缓慢释放,减少给药次数的目的。

Objective To prepare the poly（D,L-lacfic-co-glycohc acid）（PLGA）nanoparticles containing voriconazole and study their morpha and in vitro release. Methods The PLGA nanoparticles containing voriconazole were prepared by emulsion-solvent volatilization method,then observed for dispersity by laser light particle size analyzer,for morpha by scan electronic microscopy,and analyzed for drug-loading capacity and in vitro release by HPLC. Remits The peak value and distribution index of nanoparticle size were（ 126 ± 20）nm and 1.5 respectively. Under scan electronic microscope, the nanoparticles were distributed evenly, and their surfaces were smooth. The drug-loading capacity and envelopment rate of the nanoparticles were（ 1.9 ± 0.6）% and 12% respectively. From the 2nd to the 8th day after observation, the voriconazole in nanoparticles were released slowly, though burst release was observed within 24 h. Conclusion The control-released PLGA nanoparticles containing voriconazole were successfully prepared,which may reduce the times of administration.