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目的制备聚乙二醇1000维生素E琥珀酸酯(TPGS)修饰的脂质体,并对其理化性质进行考察。方法采用薄膜超声法制备脂质体,用硫酸铵梯度法制备将多柔比星载入脂质体内,阳离子交换树脂吸附法测定药物包封率,用透析法测定其体外释放,透射电镜观察脂质体形态,激光粒度测定仪测定粒度分布和Zeta电势,并考查脂质体稳定常数Ke、药物泄漏率以及胎牛血清对脂质体粒度的影响。结果 TPGS修饰的脂质体形态规整,药物包封率为(95±2.13)%(n=3);Zeta电位为-3.06mV,平均粒径为68.7 nm,多分散指数为0.186;TPGS修饰后能显著提高脂质体的贮藏以及在血清中的稳定性,大大降低药物泄漏率,而体外释放快于普通脂质体。结论 TPGS修饰的多柔比星脂质体具有包封率高、粒径小、稳定性好等优点。
OBJECTIVE To prepare liposomes modified with polyethylene glycol 1000 vitamin E succinate (TPGS) and study its physicochemical properties. Methods The liposomes were prepared by membrane ultrasonication. The drug was encapsulated in the liposomes by ammonium sulfate gradient method. The drug entrapment efficiency was determined by cation exchange resin adsorption. The release in vitro was measured by dialysis. Plastid morphology and laser particle size analyzer were used to determine the particle size distribution and Zeta potential. The liposome stability constant Ke, drug leakage rate and the effect of fetal bovine serum on liposome size were also investigated. Results The TPGS-modified liposomes had a regular shape with the encapsulation efficiency of (95 ± 2.13)% (n = 3), the Zeta potential of -3.06mV, the average particle diameter of 68.7 nm and the polydispersity index of 0.186. Can significantly improve the storage of liposomes and stability in serum, greatly reduce the drug leakage rate, and release faster than normal liposomes in vitro. Conclusion TPGS modified doxorubicin liposomes have the advantages of high entrapment efficiency, small particle size and good stability.