OBJECTIVE： To prepare Wheat germ agglutinin （WGA） modified vinorelbine （VRB） cationic liposomes （WGA-VRB cationic liposomes）， and to optimize the formulation and conduct cytotoxicity test. METHODS： Thin-film diffusion and ammonium sulfate gradient method were used to prepare WGA-VRB cationic liposomes using phospholipid and cholesterol as excipient， 3β-[N-（N′ -N′ -dimethyl aminoethane）-carbamoyl] cholesterol hydrochloride （DC-Chol） as cationic material， distearoyl phosphatidylethanolamine-polyethylene glycol 2000 （DSPE-PEG2000） as long cycle chain. Using encapsulation rate as index， central composite design-response surface methodology was used to optimize the amount of DC-Chol， cholesterol and VRB. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were determined. The effects of them and blank cationic liposomes on survival rates of human breast cancer cell MCF-7 and human non-small cell lung cancer cells A549 were compared. RESULTS： The optimal formulation of 5 mL WGA-VRB cationic liposomes was as follows as phospholipid 22 mg， cholesterol 12 mg， DC-Chol 8 mg， VRB 0.5 mg. Encapsulation rate of the liposomes was （92.24±1.21）％（n＝3）， relative error of which to predicted value was 5.3％. The contents of VRB in VRB liposomes and WGA-VRB cationic liposomes were （96.01±3.26），（93.39±1.59） μg/mL（n＝3）. Compared with blank cationic liposomes and VRB liposomes， WGA-VRB cationic liposomes could significantly reduce survival rate of MCF-7 and A549. CONCLUSIONS： WGA-VRB cationic liposomes are prepared successfully. Inhibitory effect of WGA-VRB cationic liposomes on MCF-7 and A549 cell survival is stronger than that of VRB liposomes.