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目的:研制甲氧基聚乙二醇二硬脂酰磷脂酰乙醇胺(mPEG2000-DSPE)修饰的长循环紫杉醇纳米脂质体(PEG-PTX-LP),减少市售紫杉醇制剂的不良反应并增强疗效。方法:采用薄膜超声分散法制备PEG-PTX-LP,采用激光散射粒度分析仪和透射电镜观察其物理性状,超滤法检测药物包封率,透析法检测药物缓释能力,通过细胞摄取试验观察人脐静脉内皮细胞(Human Umbilical Vein Endothelial Cells,HUVEC)、A549肺癌细胞对PEG-PTX-LP的摄取能力。结果:透射电镜显示长循环紫杉醇纳米脂质体呈圆形囊泡样结构,粒径检测其平均粒径为99.1 nm,制备后第2、7、14、21、30天的紫杉醇包封率均大于99%,在血清中的缓释能力优于泰素溶液,HUVEC、A549细胞对PEG-PTX-LP中紫杉醇的摄取量明显高于泰素溶液(Taxol)。结论:采用mPEG2000-DSPE修饰的PEG-PTX-LP具有更高的稳定性和缓释能力,对肿瘤细胞和血管内皮细胞有一定的特异性,是一种更有效的紫杉醇新剂型。
OBJECTIVE: To develop PEG-PTX-LP modified with methoxy polyethylene glycol distearoylphosphatidylethanolamine (mPEG2000-DSPE) to reduce the adverse reactions of paclitaxel in the market and to improve the curative effect . Methods: PEG-PTX-LP was prepared by thin-film ultrasonic dispersion method. The physical properties of PEG-PTX-LP were observed by laser light scattering particle size analyzer and transmission electron microscopy. Drug entrapment efficiency was measured by ultrafiltration. Human Umbilical Vein Endothelial Cells (HUVEC), A549 lung cancer cells uptake of PEG-PTX-LP. Results: Transmission electron microscopy showed that the long-circulating paclitaxel nanosomes were round vesicle-like structure. The average diameter of the paclitaxel nanosized liposomes was 99.1 nm. The encapsulation efficiency of paclitaxel at 2, 7, 14, 21 and 30 days More than 99%, and its sustained release ability in serum is better than that of taxol. The uptake amount of paclitaxel in PEG-PTX-LP by HUVEC and A549 cells was significantly higher than Taxol. CONCLUSION: PEG-PTX-LP modified with mPEG2000-DSPE has higher stability and sustained release ability and certain specificity to tumor cells and vascular endothelial cells. It is a more effective new dosage form of paclitaxel.