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目的以羟基喜树碱作为模型药物研究pH敏感阳离子纳米脂质体用于包载抗癌药物的制备工艺。方法采用薄膜分散法制备羟基喜树碱阳离子脂质体;用羧甲基壳聚糖物理修饰阳离子脂质体;用葡聚糖凝胶柱色谱法分离游离药物;用紫外分光光度法测定包封率;用单一因素考察法优选处方;经高压乳匀得到纳米脂质体(粒径小于100nm);用激光粒度分析仪测定Zeta电位、粒径大小。结果最佳处方制备的药物平均包封率为(78.5±0.9)%(n=3);包衣纳米脂质体的Zeta电位为-31.3mV,平均粒径为96nm。结论使用本方法制备pH敏感阳离子纳米脂质体工艺简单,有望获得高靶向性的抗癌药物传递系统。
OBJECTIVE To study the preparation of anticancer drug-loaded pH-sensitive cationic nanoliposomes using hydroxycamptothecin as a model drug. Methods Hydroxycamptothecin cationic liposomes were prepared by membrane dispersion method. Cationic liposomes were physically modified with carboxymethyl chitosan. Free drug was separated by dextran gel column chromatography. The encapsulation was determined by UV spectrophotometry Rate; using single factor investigation method preferred prescription; obtained by high-pressure homogenization nano-liposomes (particle size less than 100nm); laser particle size analyzer Zeta potential, particle size. Results The best encapsulation efficiency of the drug was (78.5 ± 0.9)% (n = 3). The Zeta potential of coated liposomes was -31.3mV and the average particle diameter was 96nm. Conclusion The method of preparation of pH-sensitive cationic nanosomes is simple, is expected to obtain high-targeted anti-cancer drug delivery system.