荷载紫杉醇多功能混合胶束的构建及体外评价

Preparation and in vitro evaluation of paclitaxel-loaded mixed micelles

目的以聚乙二醇维生素E琥珀酸酯(TPGS)、卵磷脂(PC)、胆酸钠(NaC)和普朗尼克F127-聚乙烯亚氨聚合物(F127-PEI)为载体制备紫杉醇混合胶束,增加其在生理条件下的稳定性和杀灭癌细胞的能力。方法采用薄膜分散法制备紫杉醇混合胶束,激光散射粒度测定仪测定粒径、Zeta电位,采用透射电镜观察外观形态,采用动态膜透析法测定体外释放情况。采用耐药的人乳腺癌细胞(MCF-7/Adr)研究胶束细胞毒性。结果紫杉醇混合胶束的平均粒径为34.8 nm,胶束多为球形,在生理条件下胶束能够保持稳定。细胞毒性结果显示,混合胶束的细胞毒性大大高于原料药。结论 F127-PEI/TPGS/NaC/PC混合胶束是一种潜在的抗癌药物给药系统。

Objective To prepare paclitaxel-loaded mixed micelles, which were made of D-α-tocopherol polyethylene glycol 1000 succinate （ TPGS）, phosphatidylcholine （ PC）, sodium cholate （NaC） and phironicF127-poly （ ethyleni- mine） （PEI）, and to investigate its characteristics and cytotoxicity against cancer cells. Methods Paclitaxel-loaded mixed micelles were prepared by film dispersion method. Zeta potential and the diameter distribution of mixed micelles were measured using laser size scattering determinator. Morphology of micelles was observed with transmission electron microscope. The release behavior of drug-loaded micelles in vitro was evaluated with dialysis method. The cytotoxicity of paclitaxel-loaded mixed micelles against MCF-7/Adr cancer cells in vitro was determined. Results The mixed mi- celles were almost spherical with an average diameter of 34.8 nm, and were stable in media modeling physiological con- ditions. The cytotoxicity against MCF-7/Adr cancer cells in vitro was remarkably higher than that of the free drug. Conclusion F127-PEI/TPGS/NaC/PC mixed micelles are a potential drug delivery system for anticancer drugs.