Objective:To prepare lactosaminated matrine liposomes and to study its targetability to liver in mice and efficacy of anti-tumor activities on human hepatoma cell line HepG2 in vitro.Methods:The matrine liposomes were prepared using the reverse-phase evaporation-ultrasonic technique.Lactosylphosphatidy-lethanolamine(Lac-PE) was synthesized and used for modified matrine liposomes..the diameter and entrapment efficiency of it were determined.The RP-HPLC was used for the determination of matrine concentration in mice tissue.The cytotoxic effect of LML on human hepatoma cell line HepG2 in vitro was detected by thiazolyl blue(MTT)assay.Results:The LML were nice and uniform

the particle diameter was between 80 and 150 nm and envelopment rats was 48.1%.Compared with matrine solution

ML and LML exhibited long circulation time.Tissue distribution results proved that the area under curve of liver was significantly difference among modified matrine liposomes

regular matrine liposomes and matrine solutions(P<0.05).The accumulation of LML in the mice liver was 2.7 times as in the spleen

3 times as in the lung

6.6times as in the kidney

and 8.5 times as in the heart(P<0.01).The inhibitory rate of LML、ML and M-sol on HepG2 ceells were 51.97%

31.89% and 28.34% at the concentrations of 0.5mg/ml

respectively.And there were markd difference between the former and the latter two(P<0.05).Conclusion:The preparation method of LML is simple and repeatable.LML showed a good liver-targeted efficiency in mice and high killing effects on hepatic carcinoma cells in vitro.