磷脂酰聚乙二醇单甲醚脂质体的制备及其载药性能  

Preparation and drug-loading property of phosphatidyl polyethyleneglycol monomethyl ether liposome

作　　者：武莉[1,2] 陈静[1,2] 刘天军[1,2] 

机构地区：[1]中国医学科学院北京协和医学院生物医学工程研究所,天津300192 [2]天津市生物医学材料重点实验室

出　　处：《国际生物医学工程杂志》2012年第6期325-328,I0003,共5页International Journal of Biomedical Engineering

基　　金：国家重大科学研究计划项目-纳米专项（2006CB933202）：教育部博士学科点基金资助项目（20070023020,20101106120052）

摘　　要：目的制备新型磷脂酰聚乙二醇单甲醚脂质体，并初步考察其载药性能和对人肺腺癌A549细胞的抗肿瘤效果。方法化学合成一系列磷脂酰聚乙二醇单甲醚，应用超声薄膜法制备脂质体和载药脂质体，测定它们的药物包封率和粒径；采用MTT法考察磷脂酰聚乙二醇单甲醚脂质体和载药磷脂酰聚乙二醇单甲醚脂质体对A549细胞增殖的影响；采用共聚焦显微镜观察脂质体在细胞中的定位。结果载紫杉醇脂质体的药物包封率约为83％；粒径范围在100～200nm；MTT实验显示载紫杉醇脂质体能显著抑制A549细胞的增殖并有长循环效果，而脂质体本身并无抑制作用。结论载药磷脂酰聚乙二醇单甲醚脂质体有缓释作用，可以开发成为新型的抗肿瘤药物载体。Objective To develop liposome loaded with paclitaxel for the treatment of lung cancer, novel phosphatidyl polyethyleneglycol monomethyl ether liposomes were prepared and studied. Methods A series of phosphatidyl polyethyleneglycol monomethyl ether liposomes were synthesized. Liposomes with or without drug were prepared by ultrasound. The entrapment efficiency and size of drug loaded liposomes were evaluated. The influence of liposomes to A549 lung cancer cell was investigated by MTT method. The cell uptake of liposome was observed by laser confocal scan microscope. Results The liposome loaded with paclitaxel had an entrapment efficiency of 83% and size of 100-200 nm.The MTT results showed phosphatidyl polyethyleneglycol monomethyl ether liposomes loaded paclitaxel have inhibition effect to A549 cells with long circulation, while liposomes without paclitaxel have not inhibition effect. Conclusion Drug loaded polyethyleneglycol monomethyl ether liposomes have sustained delivery to paclitaxel. They have potential apphcation in the therapy of cancer.

关 键 词：磷脂酰聚乙二醇单甲醚 脂质体 长循环 

分 类 号：R943[医药卫生—药剂学]