Objective         To prepare transferrin and Arg-Gly-Asp (RGD) co-modified liposomes (TF/RGD-LP) and evaluate the targeting effect to ovarian cancer in vitro and in vivo.         Methods        The RGD modified liposome (RGD-LP) was prepared by film-ultrasonic method. Transferrin and RGD co-modified liposomes (TF/RGD-LP) and the transferrin modified liposomes (TF-LP) were prepared by post-insertion method. The appearance

particle size and Zeta potential of the liposome were evaluated. The cellular uptake of these liposomes to ovarian cancer A2780 cells in vitro was determined. Then the tumor spheroids were prepared and used to evaluate the penetration efficiency of the liposome. Transplanted tumor of A2780 cells was established in nude mice

and fluorescence in vivo imaging was used to evaluate the targeting efficiency of the liposome in 12 h after injected through tail vein.         Results        The particle diameter of the co-modified liposome TF/RGD-LP was 95.5±8.7 nm with the Zeta potential of 3.05±1.25 mV. The cell uptake of TF/RGD-LP were 2.9

2.7 and 5.7 times higher than that of RGD-LP

TF-LP and LP respectively (P0.01). The evaluation of tumor spheroid penetration and in vivo imaging showed TF/RGD-LP had sound tumor targeting effect and penetration.         Conclusion        TF/RGD-LP might serve as a promising ovarian carcinoma delivery system of antitumor drugs.