In order to obtain liposomes with properties of heptocyte-specificity and pH-sensitivity, four galactosylated derivatives were synthesized. A series of liposomes were prepared by mixing the galactosylated derivatives with DC-chol/DOPE respectively. The liposome 18-gal was proven to have favorable gene transfer efficiency to human hepatoma HepG2 cells, which was significantly inhibited in the presence of galactose solution, indicating that the liposomal transfection activity was mediated by asialoglycoprotein receptors. The liposome showed prominent pH-sensitivity and low cytotoxicity. Its optimum gene transfer conditions were also determined. The results showed that the liposome may be developed as a potential hepatocyte targeting pH-sensitive delivery system for nucleic acid drugs.