羟基喜树碱pH敏感阳离子纳米脂质体的制备  

Preparation of Hydroxycamptothecin pH-Sensitive Cationic Nanoliposomes

作　　者：宋金春[1] 戎佩佩[2] 

机构地区：[1]武汉大学人民医院药学部,武汉430060 [2]武汉大学药学院,武汉430072

出　　处：《中国药学杂志》2010年第6期450-453,共4页Chinese Pharmaceutical Journal

基　　金：国家973计划项目(2009CB930301)

摘　　要：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 prepare pH-sensitive cationic nanoliposomes with hydroxycamptothecin （HCPT） as model drug. METHODS The cationic liposomes were prepared by film dispersion method. Tbe encapsulation efficiency was determined by Ultra Violet Detector. HCPT loaded within liposomes was estimated alter removing unentrapped HCPT by Sephadex - G50 chromatographic column. Carboxymethyl ehitosan was used to coat the cationic liposomes , then the liposoines were extruded through high pressure homogenizer. Zeta sizer was used to determine the Zeta potential and average size of the HCPT liposomes. RESULTS The size of liposomes was around 96 nm and drug encapsulation efficiency was 78.5%. CONCLUSION The preparation of this stable, long circu- lating pH-sensitive cationic HCPT containing nanoliposomes are easy to prepare and the drug concentration of pH-sensitive cationic nanoliposomes in tumor cells was remarkably higher than that of free drug.

关 键 词：PH敏感 阳离子 长循环 纳米脂质体 

分 类 号：R944[医药卫生—药剂学]