Transarterial Chemoembolization Using Docetaxel-Loaded Phytantriol Cubic Phase Precursor for the Treatment of Hepatocellular Carcinoma

The purpose of this study was to evaluate the transarterial chemoembolic agent based on docetaxel-loaded phytantriol cubic phase precursor (DTX PCPP) by in vitro cytotoxicity study and in vivo evaluation of antitumor efficacy as well as the histological examination. The methythiazolyl tereazolium bromide assay in Hep G2 cell line revealed that DTX PCPP generated high cytotoxicity by causing cell apoptosis and G2/M phase arrest. In vivo studies conducted in rabbits bearing VX2 tumors, which were treated with DTX PCPP, used as a transarterial chemoembolic agent, showed a significant antitumor efficacy and prominent higher DTX concentrations in tumor and liver than those in other organs. The histology presented typical necrosis in tumor that demonstrated excellent therapeutic effect. In conclusion, the DTX PCPP could achieve an excellent antitumor effect with low systemic toxicity for the treatment of hepatocellular carcinoma and therefore implied the prospect of DTX PCPP for clinical applications. (C) 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:2240-2247, 2011