一种肝细胞靶向pH敏感脂质体的制备及性质分析
Preparation and property analysis of a hepatocyte targeting pH-sensitive liposome.
作者信息
Wen Si-Yuan, Wang Xiao-Hong, Lin Li, Guan Wei, Wang Sheng-Qi
机构信息
Beijing Institute of Radiation Medicine, Beijing 100850, China.
出版信息
World J Gastroenterol. 2004 Jan 15;10(2):244-9. doi: 10.3748/wjg.v10.i2.244.
AIM
To develop a hepatocyte targeting pH-sensitive liposome for drug delivery based on active targeting technology mediated by asialoglycoprotein receptors.
METHODS
Four types of targeting molecules with galactose residue were synthesized and mixed with pH-sensitive lipids DC-chol/DOPE to prepare liposome with integrated property of hepatocyte specificity and pH sensitivity. Liposome 18-gal was selected with the best transfection activity through cellular uptake experiment. Property analysis was made through experiments of competitive inhibition of receptors, red blood cell hemolysis, in vitro cytotoxicity test by MTS assay and mediation of inhibitory effects of antisense phosphorothioate ODN on gene expression, etc.
RESULTS
Liposome 18-gal had the desired properties of hepatocyte specificity, pH sensitivity, low cytotoxicity, and high transfection efficiency.
CONCLUSION
Liposome 18-gal can be further developed as a potential hepatocyte- targeting delivery system.
目的
基于去唾液酸糖蛋白受体介导的主动靶向技术，开发一种用于药物递送的肝细胞靶向pH敏感脂质体。
方法
合成四种带有半乳糖残基的靶向分子，并与pH敏感脂质DC-胆甾醇/二油酰磷脂酰乙醇胺混合，制备具有肝细胞特异性和pH敏感性综合特性的脂质体。通过细胞摄取实验选择转染活性最佳的脂质体18-半乳糖。通过受体竞争性抑制实验、红细胞溶血实验、MTS法体外细胞毒性试验以及反义硫代磷酸酯寡核苷酸对基因表达抑制作用的介导等实验进行性质分析。
结果
脂质体18-半乳糖具有所需的肝细胞特异性、pH敏感性、低细胞毒性和高转染效率等特性。
结论
脂质体18-半乳糖可进一步开发成为一种潜在的肝细胞靶向递送系统。
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