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以叶酸-聚乙二醇-二硬脂酰磷脂酰乙醇胺(FA-PEG 3350-DSPE)和甲氧基聚乙二醇-二硬脂酰磷脂酰乙醇胺(mPEG 2000-DSPE)(摩尔比1∶100)作为混合载体材料,采用固体分散-水化法,制备包载紫杉醇(1)的聚合物胶束,以星点设计-效应面法进行处方优化,并考察了聚合物胶束的理化性质、体外抑制肿瘤细胞生长效果及对巨噬细胞摄取的影响。结果表明,优化所得胶束的包封率为81%、载药量为2.7%、平均粒径为12～16 nm,可持续释放24 h;制品可有效提高1体外抑制肿瘤细胞生长的效果,加入1%的FA-PEG 3350-DSPE可略减弱mPEG 2000-DSPE规避巨噬细胞吞噬的效果。
(FA-PEG 3350-DSPE) and methoxypolyethylene glycol-distearoylphosphatidylethanolamine (mPEG 2000-DSPE) at a molar ratio of 1: 100) as a mixed carrier material, the polymer micelles coated with paclitaxel (1) were prepared by solid dispersion-hydration method. The formulation design was optimized by the method of star design-response surface methodology. The physicochemical properties , In vitro inhibition of tumor cell growth and macrophage uptake. The results showed that the encapsulation efficiency of the optimized micelles was 81%, the drug loading was 2.7%, the average particle size was 12 ~ 16 nm and sustained release was 24 h. The products could effectively enhance the effect of inhibiting the growth of tumor cells in vitro, The addition of 1% FA-PEG 3350-DSPE slightly diminished the effect of mPEG 2000-DSPE to evade macrophage phagocytosis.