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 micrograms.ml-1 and 0.34 micrograms.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.