Formula Optimization of Evodiamine Liposomes by Central Composite Design-Response Surface Methodol-ogy / 中国药师

ABSTRACT

Objective:To optimize the formula of evodiamine liposomes. Methods:Using phospholipids, cholesterol and vitamin E as the materials, the liposomes were prepared by a film dispersion method. The binomial model of mass ratio of phospholipid to drug, mass ratio of phospholipid to cholesterol and the concentration of phospholipid were fitted by design-response surface methodology using encapsulation efficiency as the index. The formula was optimized by three-dimensional response surface and contour plot. The predic-tive data was validated, and the morphology, particle size and pH were observed. Results:The optimized formula was as followsthe mass ratio of phospholipid to drug was 30. 58∶1, that of phospholipid to cholesterol was 15. 22∶1 and the concentration of phospholipid was 42. 26 mg·ml-1 . The average encapsulation efficiency of evodiamine liposomes was 92. 89%. The appearance was milky white and translucent with round or oval pellets, the particle size was 126 nm and the pH was 6. 94 ± 0. 17. Conclusion: The formula and preparation process of evodiamine liposomes are stable and feasible.