Abstract: Objective To prepareRGD and TAT co-modified paclitaxel loaded liposome（RGD/TAT-LP-PTX）for HepG2cells targeting．Methods The co-modified liposome was prepared by film-ultrasonic method. The appearance，particle size，Zeta potential were evaluated. The cellular uptake by HepG2cellsin vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/TAT-LP-PTX was evaluated by MTT assay. Results The particle diameter of the co-modified liposome was 134.5±8.4 nm with the Zeta potential of 22.35±2.55mV. The entrapment efficiency of PTX was 84.6%. The result demonstrated that the co-modified liposome uptaken by HepG2 were 2.2, 2.7 times higher than that of TAT-LP and RGD-LP, respectively.The MTT assay demonstrated the cell viability of TAT-LP-PTX，RGD-LP-PTX and LP-PTX were 1.65, 1.74 and 2.1 times higher than that of RGD/TAT-LP-PTX respectively. Conclusion: The co-modified liposome might serve as a promising tumor delivery system of antitumor drugs.

Key words: Integrin receptor, Cell penetrating peptides, liposomes, tumor targeting