OBJECTIVE: To establish the method for the determination of main components content and entrapment efficiency of transferrin modified vincristine-tetrandrine liposomes. METHODS: HPLC method was adopted to determine the content of vincristine. The determination was performed on ELITE C18 column with mobile phase consisted of methanol-15% triethylamine (70 ∶ 30) at a flow rate of 1.0 ml/min. The determination wavelength was set at 297 nm and column temperature was 30 ℃. The sample size was 20 μl. Free drug was isolated from liposomes by dextran gel column chromatography, and entrapment efficiency was determined. RESULTS: The linear range of vincristine was 160-1 600 μg/ml (r=0.999 8, n=5) with average recovery of 99.20% (RSD=0.26%, n=9). RSD of precision test was 0.070% (n=5). The average content of vincristine in liposomes was 0.790 mg/ml (RSD=0.15%, n=3), and the average entrapment efficiency was 85.94% (RSD=2.08%, n=3). CONCLUSIONS: The method is accurate, reliable, simple and rapid, and can be used for the determination of the content and entrapment efficiency of vincristine in transferrin modified vincristine-tetrandrine liposomes.