Liposomal Brucine (LB) with high encapsulation efficiency (72%) and small particle diameter (mean particle diameter, 54 nm) was prepared by ethanol-dripping method. The safety and pharmacodynamic action of LB, a new transdermal preparation, were investigated in details with the use of white rabbits, guinea-pigs and mice, respectively. The tests revealed that LB had no acute toxicity to integral and broken skin, and had no allergic effects on skin. In writhing test, the analgesic effect of LB was higher than that of free brucine. The anti-inflammatory activity of LB was significantly higher than that of free brucine (P<0.01). Meanwhile, LB exhibited a better dose-response manner and a longer duration of analgesic effects. In conclusion, LB could reduce the toxicity of brucine, enhance the analgesic and antiinflammatory effects of brucine, and achieve its sustained-release.