紫杉醇磁性脂质体的制备与抗肿瘤作用研究

Preparation of Paclitaxel Magnetic Nanoparticle Liposome and Anti-tumor Activity

目的制备紫杉醇磁性纳米脂质体,并研究其对3种肿瘤细胞的抑制效果。方法应用超声薄膜分散法制备紫杉醇磁性纳米脂质体,通过正交设计来优化制备工艺,噻唑蓝(MTT)法研究其对肿瘤细胞的抑制效果。结果最佳处方和工艺条件为:磷脂酰胆碱:胆固醇为4:1,紫杉醇:(磷脂酰胆碱+胆固醇)为1:30,超声处理时间30min,磁粉:紫杉醇为1:1,聚山梨酯-80:紫杉醇为4:1,聚乙二醇1000:紫杉醇为8:1;制备的紫杉醇磁性纳米脂质体包封率约85.8%,平均粒径约150nm;对3种肿瘤细胞均有良好的抑制效果,并呈现一定的缓释作用。结论该方法制备的紫杉醇磁性纳米脂质体包封率较高,分布均匀,对3种肿瘤细胞抑制效果较好,符合靶向制剂的要求。

Objective To prepare the paclitaxel magnetic nanoparticle liposome,and investigate its anti-tumor activity in vitro.Methods It was prepared by using membrane ultrasound disintegration method,which was optimized by orthogonal design,and the in vitro anti-tumor activity was investigated by MTT method.Results The best preparation and formulation were as follows：lecithin：cholesterol=4：1,paclitaxel：（lecithin＋cholesterol）=1：30,ultrasounding for 40 min,magneticpowder：paclitaxel=1：1,tween-80：paclitaxel=4：1,polyethylene-1 000：paclit-axel =8：1.The average encapsulation efficiency of the optimized liposome was 85.8%,the average particle size was 150 nm.Its anti-tumor activity on three types of cancer cells was good and with sustained release property.Conclusion The paclitaxel magnetic nanoparticle liposome prepared by thin film ultrasonic method has a high encapsulation efficiency,evenly distribution,and potent anti-tumor activity,which meets the requirements for targeting preparation.