聚乳酸-羟基乙酸聚合物载入羟基喜树碱载药纳米粒子的制备及表征

以抗癌药物羟基喜树碱作为模型药物,可降解材料聚乳酸-羟基乙酸(PLGA)为药物负载体,采用溶剂-抗溶剂沉淀法制备聚乳酸-羟基乙酸/羟基喜树碱的载药纳米微球,考察不同溶剂-反溶剂体系对载药包封效果的影响。结果表明,以丙酮-水为溶剂体系制备的载药微球性能较好,形貌外观呈圆球形,球表面圆润光滑,粒度均一,分散效果良好,平均粒径为160 nm,载药微球包封率随着载药量的增加而减小,实测载药量为7.83%的PLGA载药微球,其载药包封率为87.68%,在28 d后溶出累计量约50%,可见以聚乳酸-羟基乙酸为载体制备的羟基喜树碱剂型,缓释作用良好。

Preparation and Characterization of Poly(lactic-co-glycolic acid) Nanoparticles Containing Hydroxycamptothecin

The poly(lactic-co-glycolic acid) (PLGA)nano-microspheres containing hydroxycamptothecin (HCPT) was prepared using solvent and anti-solvent precipitation method with HCPT as the model drug, degradable PLGA as the carrier. The effects of different solvents and anti-solvents system on the drug loading capacity andentrapment efficiency were investigated. The results showed that the microspheres prepared with acetone-water as solvent system had better performance, spherical appearance, round and smooth surface, uniform particle size (the average particle size of 160 nm) and good dispersion. The entrapment efficiency of drug-loaded microspheres decreased with the increase of drug loading.It was found that theentrapment efficiency was 87.68% in the HCPT/PLGA microspheres when drug loading was 7.83%. The cumulative release amount was 50% after 28 days. This HCPT/PLGA drug delivery system clearly demonstrated its good sustained-release effect.