RGD和细胞穿膜肽共修饰脂质体的构建及其体外功能评价

基础医学与临床 ›› 2014, Vol. 34 ›› Issue (8): 1083-1087.

RGD和细胞穿膜肽共修饰脂质体的构建及其体外功能评价

赵炳芬

胜利油田中心医院肿瘤科

收稿日期:2013-12-24 修回日期:2014-03-22 出版日期:2014-08-05 发布日期:2014-07-15
通讯作者: 赵炳芬 E-mail:527236911@qq.com

The preparation and characterization of RGD and the function of cell penetrating peptides co-modified paclitaxel loaded liposome in vitro

Received:2013-12-24 Revised:2014-03-22 Online:2014-08-05 Published:2014-07-15

摘要/Abstract

摘要： 目的制备RGD和TAT共修饰载紫杉醇（PTX）脂质体（RGD/TAT-LP-PTX），研究其理化性质和体外抗肿瘤作用。方法薄膜分散法制备RGD/TAT-LP-PTX，研究其理化性质；检测肝癌HepG2细胞对RGD/TAT-LP的摄取效率以及脂质体的摄取机制。共聚焦实验研究肿瘤细胞对脂质体的摄取。MTT检测RGD/TAT-LP-PTX对HepG2细胞的增殖抑制作用。结果 RGD/TAT-LP-PTX的粒径134.5±8.4 nm，电位为22.35±2.55 mV，紫杉醇的包封率84.6%。RGD/TAT-LP在4 h摄取效率是2 h的1.65倍（P<0.05）；HepG2细胞在4 h对RGD/TAT-LP的摄取效率分别是TAT-LP、RGD-LP和LP的2.2倍、2.7倍和3.9倍（P<0.01）；RGD/TAT-LP-PTX在24 hHepG2细胞的存活率是48 h的1.75倍（P<0.05）；给药48 h后，TAT-LP-PTX、RGD -LP-PTX和LP-PTX的细胞存活率分别是RGD/TAT-LP-PTX组的1.65倍、1.74倍和2.1倍（P<0.01）。结论 RGD和TAT共修饰紫杉醇脂质体是一种潜在高效的肿瘤靶向给药系统。

关键词: 整合素受体, 细胞穿膜肽, 脂质体, 肿瘤靶向

Abstract: Objective To prepareRGD and TAT co-modified paclitaxel loaded liposome（RGD/TAT-LP-PTX）for HepG2cells targeting．Methods The co-modified liposome was prepared by film-ultrasonic method. The appearance，particle size，Zeta potential were evaluated. The cellular uptake by HepG2cellsin vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/TAT-LP-PTX was evaluated by MTT assay. Results The particle diameter of the co-modified liposome was 134.5±8.4 nm with the Zeta potential of 22.35±2.55mV. The entrapment efficiency of PTX was 84.6%. The result demonstrated that the co-modified liposome uptaken by HepG2 were 2.2, 2.7 times higher than that of TAT-LP and RGD-LP, respectively.The MTT assay demonstrated the cell viability of TAT-LP-PTX，RGD-LP-PTX and LP-PTX were 1.65, 1.74 and 2.1 times higher than that of RGD/TAT-LP-PTX respectively. Conclusion: The co-modified liposome might serve as a promising tumor delivery system of antitumor drugs.

Key words: Integrin receptor, Cell penetrating peptides, liposomes, tumor targeting

赵炳芬. RGD和细胞穿膜肽共修饰脂质体的构建及其体外功能评价[J]. 基础医学与临床, 2014, 34(8): 1083-1087.

[1]	权毅. 转铁蛋白修饰共载阿霉素与蒽贝素脂质体的构建及其体外评价[J]. 基础医学与临床, 2014, 34(11): 1548-1552.
[2]	邓益斌张梁王燕菲. HBV S基因反义锁核酸抑制病毒体外复制[J]. 基础医学与临床, 2010, 30(4): 360-363.
[3]	陈巾杰浦晓东. TIMP-3基因瞬时表达对兔血管平滑肌细胞增殖、迁移及凋亡的影响[J]. 基础医学与临床, 2008, 28(7): 756-759.