Objective      To prepare liposomes co-modified by transferrin and Arg-Gly-Asp (RGD) and to evaluate their glioma-targeting efficiency

in vitro

and

in vivo

.       Methods      The co-modified liposome was prepared by film-ultrasonic method. The appearance

particle size

and Zeta potential were evaluated. The cellular uptake by U87 cells

in vitro

and

in vivo

imaging were used to evaluate the targeting efficiency.       Results      The particle diameter of the co-modified liposome was 120.0±8.5 nm with the Zeta potential of -5.00±1.15 mV. The results demonstrated that the co-modified liposome uptaken by U87 were 2.1 and 2.7 time

s higher than that of transferrin-modified liposome and RGD-modified liposome

respectively. The evaluation of tumor spheroid penetration and

in vivo

imaging showed the co-modified liposome had the strongest fluorescence intensity.       Conclusion      The co-modified liposome might serve as a promising glioma delivery system of antitumor drugs.