OBJECTIVE：To prepare transferrin modified paclitaxel-loaded liposome（TF-PTX-LP），and to study the tumor inhibition effect. METHODS：TF-PTX-LP was prepared by thin-film method，and morphology of TF-PTX-LP was observed. Qualitative and quantitative investigation were used to value the uptake efficiency of TF-LP and LP by HepG2 cells. The proliferation inhibition rate of HepG2 cells was investigated after treated with PTX，PTX-LP and TF-PTX-LP for 24，48 and 72 h. Tumor spheres were prepared by using HepG2 cells. Effects of normal saline，PTX，PTX-LP and TF-PTX-LP on the volume of tumor spheres were investigated after 0，1，2，4，5，6 and 7 d treatment. HepG2 tumor-bearing nude mice model was induced. Inhibitory effects of normal saline，PTX，PTX-LP and TF-PTX-LP（8.5 mg/kg by PTX）on transplantable tumor of tumor-bearing nude mice were investigated. RESULTS：TF-PTX-LP showed uniform spherical shape，with particle size of 100-120 nm. The fluorescence intensity of HepG2 cells treated with TF-LP was stronger than that treated with LP（P＜0.01）. Compared with PTX and PTX-LP，TF-PTX-LP showed higher proliferation inhibition rate（P＜0.01）. Compared with normal saline，PTX and PTX-LP，tumor spheres were smaller in volume after treated with TF-PTX-LP，and inhibition rate of tumor was higher in tumor-bearing nude mice；there were statistical significance after treated for 6，7 d（P＜0.01）. The proliferation inhibition rate and tumor spheres volume changed in time-dependent manner. CONCLUSIONS：TF-PTX-LP which owns good tumor inhibition effect is prepared successfully.