Preparation of 5-Fluorouracil and Ampelopsin Compound Liposome

OBJECTIVE To study the preparation of 5-fluorouracil and ampelopsin compound liposome and to establish a ultraviolet spectroscopy for simultaneous determination of the two drugs. METHODS Based on the test of single factors, the optimized formulation of compound liposome was obtained by the orthogonal methodology. Entrapment ratio and diameter of the liposome were served as index. The entrapment efficiency of compound liposome was determined by means of Sephadex gel chromatography. The contents of 5-fluorouracil and ampelopsin were determined by ultraviolet spectroscopy. RESULTS Ultraviolet spectrophotometry was used for analyzing the amount of 5-fluorouracil and ampelopsin. The recovery of 5-fluorouracil and ampelopsin was in a range of 99%-102%. The compound liposomes were prepared by the film-dispersion- ultrasonic technique. The best craft produce was investigated by single factor and the optimal preparation conditions were as follows: drug∶lecithin=1∶20, lecithin∶cholesterol=4∶1, phospholipid concentration 50 g·L^-1, vitamin E 5%, pH 7.4 phosphate buffer 16 mL. The entrapment efficiencies of 5-fluorouracil and ampelopsin of compound liposome were (44.79±1.55)% and (75.47±0.91)% (n=3) , and the particle size was (142±3.6)nm. The in vitro 12 h accumulative release of 5- fluorouracil and ampelopsin were 43.05% and 60.24% of the total drug. CONCLUSION Film-dispersion-ultrasonic technique for the compound liposome preparation is simple and efficiency. Compound liposome has high entrapment efficiency and the quality of the liposome is controllable. This ultraviolet spectroscopy can be used for quality control of 5-fluorouracil and ampelopsin in the compound liposome.