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

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

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。

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,degradablePLGA as the carrier.The effects of different solvents and anti-solvents system on the drug loading capacityand entrapment efficiency were investigated.The results showed that the microspheres prepared withacetone-water as solvent system had better performance,spherical appearance,round and smooth surface,uniform particle size(the average particle size of160nm)and good dispersion.The entrapment efficiency ofdrug-loaded microspheres decreased with the increase of drug loading.It was found that the entrapmentefficiency was87.68%in the HCPT/PLGA microspheres when drug loading was7.83%.The cumulativerelease amount was50%after28days.This HCPT/PLGA drug delivery system clearly demonstrated itsgood sustained-release effect.