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采用聚(乳酸羟基乙酸)共聚物(PLGA)纳微球装载紫杉醇,并用壳聚糖季铵盐(HTCC)对PLGA微球表面进行镀层修饰,比较了修饰前后载药微球的形貌、粒径、电位、载药率、释药行为和细胞杀伤效果.结果表明,修饰后微球表面圆整光滑,平均粒径为882nm,载药率可达5.15%,包埋率达70.46%,体外释药22d累积释药率为70.17%,与修饰前没有显著性差异;但修饰后微球表面电荷由修饰前的14.8mV翻转为+36.7mV,肿瘤细胞对PLGA和HTCC-PLGA载药微球的内吞量分别是Taxol的5.6和9.7倍,且HTCC-PLGA载药微球对细胞杀伤效果显著,是一种有潜力的难溶性药物递送系统.
PLGA nanospheres were loaded with paclitaxel, and the surface of PLGA microspheres was modified with chitosan quaternary ammonium salt (HTCC). The morphologies of the loaded microspheres before and after modification were compared Diameter, potential, drug loading rate, drug release behavior and cell killing effect.The results showed that the modified microspheres were round and smooth, the average particle size was 882nm, the drug loading rate was 5.15%, the embedding rate was 70.46% The released drug release rate of 22d was 70.17%, which was not significantly different from that before modification. However, the surface charge of the modified microspheres turned to + 36.7mV from 14.8mV before modification, and the PLGA and HTCC-PLGA drug loaded microspheres Were 5.6 and 9.7 times higher than that of Taxol, respectively. Moreover, HTCC-PLGA drug-loaded microspheres had a significant cytotoxic effect on cells, which was a potential drug delivery system with poor solubility.