反义寡核苷酸／司盘修饰阳离子脂质体复合物的制备和特性  

Preparation and characterization of cationic liposomes complex modified by antisense oligonucleotides/Span

作　　者：黄永焯[1] 陈海靓[1] 陈金亮[1] 梁文权[1] 

机构地区：[1]浙江大学药物制剂研究所,浙江杭州310031

出　　处：《中国药学杂志》2005年第24期1880-1883,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金(30371692)

摘　　要：目的 通过采用司盘系列表面活性剂对阳离子脂质体进行修饰,以提高基因传递效率,寻找高效的基因载体。方法 采用逆相蒸发法制备司盘阳离子脂质体。通过静电作用,得到反义寡核苷酸／阳离子脂质体自组装复合物,并运用电镜、激光 粒度及Zeta电位测定、琼脂糖电泳和荧光光谱等技术手段对司盘阳离子脂质体和自组装复合物进行了物理表征。并在体外 培养细胞系——COS7和RKO进行了摄取实验,对此载体进行生物学评价。结果 体外细胞摄取实验表明,司盘阳离子脂质 体与普通阳离子脂质体相比,可提高细胞对反义寡核苷酸的摄取,司盘40修饰阳离子脂质体效果最为显著。结论 采用表面 活性剂司盘修饰是提高基因传递效率切实可行的方法。表面活性剂司盘修饰阳离子脂质体为颇具发展潜力的非病毒载体。OBJECTIVE To develop a potential gene delivery system, to investigate the surface modification of cationic liposomes with surfactants-Span series for facilitating gene transfer.METHODS Span-cationic liposomes were prepared by reverse phase evaporation method. Antisense oligonucleotides/surfaetant modified cationic liposomes self-assemble complex was prepared by auto-coacervation. Spancationic liposomes and self-assemble complex were characterized by morphology, particle size, Zeta potential, agarose electrophoretic retarding and fluorescence spectra. And the celluar uptake of antisense oligonucleotides mediated by different Span modified cationic liposomes by COS7 ＆ RKO cell lines was studied. RESULTS The study of cellular uptake in vitro showed that Span played a role in enhancing the cellular uptake of OND by COS7 ＆ RKO cell lines. The cationic liposomes modified by Span 40 significantly facilitated the cellular uptake by both tested lines. CONCLUSION The surface modification of cationic liposomes with surfactants Span can be a way to enhance the efficiency of gene transfer. And Span-cationic liposome can be a potential gene vector.

关 键 词：阳离子脂质体 反义寡核苷酸 表面活性剂 司盘 基因载体 

分 类 号：R943.4[医药卫生—药剂学]