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阳离子脂质材料和聚乙二醇对脂质体细胞转染率及膜流动性的影响

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

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【作者】 严文伟齐宪荣魏来费然丛旭王宇

【Author】 YAN Wen wei 1, QI Xian rong 1* , WEI Lai 2, FEI Ran 2, CONG Xu 2, WANG Yu 2 (1. Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China; 2. Institute of Hepatology, People’s Hospital, Peking University, Beijing 100044, China)

【机构】 北京大学药学院药剂系北京大学人民医院肝病研究所北京大学人民医院肝病研究所 北京100083北京100083北京100044北京100044

【摘要】 目的 制备包封荧光素钠 (FS)的脂质体 ,考察阳离子脂质材料 (DC chol)和聚乙二醇 (PEG)对脂质体包封率、细胞转染率及膜流动性的影响。方法 以FS作为模型物质 ,制备并分离脂质体 ,测定脂质体包封率 ;通过观察荧光光谱的变化考察FS与脂质体膜之间的相互作用 ;以HepG2 2 .2 .15为细胞模型观察脂质体对FS细胞转染率的影响 ;通过荧光偏振技术考察阳离子脂质材料和PEG对脂质体膜流动性的影响。结果 阳离子脂质材料和PEG能提高脂质体包封率 ( 0 6 4 %~ 86 5 7% )、细胞转染率 ( 2 18%~ 4 8 4 6 % )及脂质体膜流动性 ,PEG分子质量的增大有利于包封率、转染率的提高 ,并增加脂质体膜的流动性。结论 在脂质体处方中加入阳离子脂质材料和高分子量的PEG有利于提高包封率、细胞转染率及增加脂质体膜的流动性

【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×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 HepG 2 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 increaseing 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.

  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2003年09期
  • 【分类号】R944
  • 【被引频次】1
  • 【下载频次】282
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