OBJECTIVE: To prepare the vinorelbine-tetrandrine liposomes modified with RGD, and study the inhibitory effect on glioma C6 cells. METHODS: Film dispersion method and ammonium sulfate gradient method were used to prepare the vinorelbine-tetrandrine liposomes modified with RGD, and the morphology and particle size distribution were observed. The vinorelbine content was determined, and sulforhodamine B method was used to respectively determine the inhibitory effects of blank targeting liposomes, normal vinorelbine liposomes and vinorelbine-tetrandrine liposomes modified with RGD on C6 cells. RESULTS: The prepared vinorelbine-tetrandrine liposomes modified with RGD were spherical or almost spherical with smooth surface, and particle size was about 120 nm. The average content of vinorelbine was 28.27 μg/mL (RSD=0.38%, n=3). Blank targeting liposomes had no significant effect on the growth of C6 cells; vinorelbine-tetrandrine liposomes modified with RGD can obviously inhibit the growth of C6 cells, and cell viability after its effect was significantly lower than normal vinorelbine liposomes (P<0.05). CONCLUSIONS: Vinorelbine-tetrandrine liposomes modified with RGD are successfully prepared, and they show obvious inhibitory effects on the growth of C6 cells.