Abstract: This paper reports the results of experiments on the antihepatoma effects of live targeted drug delivery system—lyophilized aclacinomycin A polyisobutylcyanoacrylate nanoparticle(ACM-IBC-NP )in vitro and in vivo. The median inhibition concentration were found to be 0.28 μg·ml-1 and 0.34μg·ml^-1 of lyophilized ACM-IBC-NP and ACM respectively in vitro. The inhibition ratio of colony formation were found to be 99%and 88%of lyophilized ACM-IBC-NP and ACM respectively in vitro,The antihepatoma activity was shown to be significantly concentration dependent.The results showed that lyophilized ACM-IBC-NP and ACM possess strong cytotoxicity on human hepatoma cell 7703,and the cytotoxicity was not significantly different between lyophilized ACM-IBC-NP and ACM in vitro. The model of orthotopic transplantation of human hepatoma in nude mice were used for evaluation of the activity of lyophilized ACM-IBC-NP against hepatoma. The tumor inhibition rate were found to be 86.84%for lyophilized ACM-IBC-NP and 46.69%for ACM. The cell proliferative activity of hepatoma were found to be 20.83%by lyophilized ACM-IBC-NP and 72.50%by ACM;All the results indicate that lyophilized ACM-IBC-NP and ACM have clinical application potential and the antihepatoma activity of lyophilized ACM-IBC-NP was obviously higher than that of ACM.