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阳离子脂质与聚乙二醇增强脂质体介导的细胞转染并增加脂质体膜的流动性

[Cationic lipid and polyethylene glycol enhance liposomes-mediated cell transfection and increase the fluidity of liposomes membranes].

作者信息

Yan Wen-wei, Qi Xian-rong, Wei Lai, Fei Ran, Cong Xu, Wang Yu

机构信息

Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China.

出版信息

Yao Xue Xue Bao. 2003 Sep;38(9):698-701.

Abstract

AIM

To prepare fluorescein sodium (FS) cationic liposomes and investigate the influence of cationic lipid (DC-chol) and polyethylene glycol (PEG) with different molecule weight (MW) on cationic liposome incorporation efficiency, cellular delivery and fluidity of liposome membrane.

METHODS

Using FS as a model material for encapsulation, the liposomes were prepared and separated (by sephadex G-50 1 cm x 20 cm column), and the liposome incorporation efficiencies was measured. The interaction between the FS and cationic liposomes was investigated by measuring the change of fluorescent spectrum. The cellular uptake of different liposome forms by choosing HepG2 2.2.15 as an in vitro cell culture assay model, and the influence of PEG on the fluidity of liposome membrane with the technique of fluorescence polarization were investigated.

RESULTS

Cationic lipid and different PEGs showed great effects on increasing liposome incorporation efficiency (from 0.64% to 86.57%), cellular uptake (from 2.18% to 48.46%) and fluidity of liposome membrane. The effect of PEG was MW dependent, and with the increase of MW, the incorporation efficiency and transfection was improved, and the fluidity of liposome membrane increased.

CONCLUSION

Addition of cationic lipid and high MW PEG into cationic liposomes can enhance the cellular delivery and fluidity of cationic liposomes. Also, they can improve the incorporation efficiency of cationic liposomes.

摘要

目的

制备荧光素钠(FS)阳离子脂质体,研究阳离子脂质(DC-胆甾醇)和不同分子量(MW)的聚乙二醇(PEG)对阳离子脂质体包封率、细胞递送及脂质体膜流动性的影响。

方法

以FS作为包封的模型材料,制备脂质体并进行分离(通过葡聚糖G-50 1 cm×20 cm柱),测定脂质体包封率。通过测量荧光光谱的变化研究FS与阳离子脂质体之间的相互作用。选用HepG2 2.2.15作为体外细胞培养测定模型,研究不同脂质体形式的细胞摄取情况,并采用荧光偏振技术研究PEG对脂质体膜流动性的影响。

结果

阳离子脂质和不同的PEG对提高脂质体包封率(从0.64%提高到86.57%)、细胞摄取(从2.18%提高到48.46%)及脂质体膜流动性有显著影响。PEG的作用取决于分子量,随着分子量的增加,包封率和转染率提高,脂质体膜流动性增加。

结论

向阳离子脂质体中添加阳离子脂质和高分子量PEG可增强阳离子脂质体的细胞递送能力和流动性,还可提高阳离子脂质体的包封率。

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