OBJECTIVE： To study the targeting of folic acid （FA）-modified docetaxel （DOC） nano-liposome （L-DOC-FA） to hepatocellular carcinoma Bel-7402 cells in vivo and in vitro. METHODS： The cell viability and survival rate of Bel-7402 cells was tested by CCK-8 kit after treated with 0， 1， 2， 5， 10 and 20 μg/ml DOC， L-DOC and L-DOC-FA for 24 h. And then， the fluorescein isothiocyanate was used to label L-DOC and L-DOC-FA nano-liposome， and the rate of L-DOC and L-DOC-FA absorbed by hepatocellular carcinoma Bel-7402 cells were detected. 125I was used to label L-DOC and L-DOC-FA nano-liposome， and then the contents of them in the subcutaneous tumor tissues were detected. 28 Balb/c naked mice were selected and given liver cell suspension via back ih to induce tumor model. After modeling， naked mice were divided into blank control group （normal saline）， DOC group （3 mg/kg）， L-DOC （3 mg/kg， by DOC） and L-DOC-FA （3 mg/kg， by DOC）. They were given relevant medicine intravenously once a day for consecutive 30 d. The relative tumor volume in naked mice was detected. RESULTS： DOC， L-DOC and L-DOC-FA all inhibited the cell viability of Bel-7402 cells， the survival rate of cells decreased in concentration-dependant manner； compared with DOC and L-DOC， the cell viability decreased after treated with L-DOC-FA， the survival rate of cells decreased （P＜0.01）. The rate of L-DOC and L-DOC-FA absorbed by Bel-7402 cells in descending order as L-DOC-FA （69.5％）＞L-DOC （31.2％）， with statistical significance （P＜0.01）. The content of L-DOC-FA in tumor was significantly more than that of L-DOC （P＜0.01）. In addition， 3 mg/kg L-DOC-FA showed better inhibitory effect than 3 mg/kg L-DOC and DOC on tumor， and the relative tumor volume was smaller （P＜0.01）. CONCLUSIONS： L-DOC-FA has obvious targeting to Bel-7402 cells in vivo and in vitro， and shows good inhibitory effect on tumor in vivo and in vitro.