Basic Research
Copyright ©The Author(s) 2004. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Jan 15, 2004; 10(2): 244-249
Published online Jan 15, 2004. doi: 10.3748/wjg.v10.i2.244
Preparation and property analysis of a hepatocyte targeting pH-sensitive liposome
Si-Yuan Wen, Xiao-Hong Wang, Li Lin, Wei Guan, Sheng-Qi Wang
Si-Yuan Wen, Xiao-Hong Wang, Li Lin, Wei Guan, Sheng-Qi Wang, Beijing Institute of Radiation Medicine, Beijing 100850, China
Author contributions: All authors contributed equally to the work.
Supported by the grants of the State 863 High Technology Project of China, No. 102-08-04-01
Correspondence to: Professor Sheng-Qi Wang, Beijing Institute of Radiation Medicine, No. 27 Taiping Road, Beijing 100850, China. sqwang@nic.bmi.ac.cn
Telephone: +86-10-66932211 Fax: +86-10-66932211
Received: April 2, 2003
Revised: May 27, 2003
Accepted: June 4, 2003
Published online: January 15, 2004
Abstract

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.

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