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目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,磷脂与胆固醇比例为12∶1,脂药比为15∶1,DSPEMPEG2000摩尔百分比为5%。此条件下制备的脂质体包封率为90.6%,平均粒径为113.4 nm,Zeta电位为-45.9 m V。结论:本实验所制备的呋喃二烯长循环脂质体包封率较高,粒度分布范围较窄,平均粒径较小,具有很好的应用前景。
OBJECTIVE: To prepare and characterize furadiglipine long-circulating liposomes. Methods: Furanodiene long - circulating liposomes were prepared by ultrasonic dispersion method. The encapsulation efficiency and particle size were used as evaluation indexes to optimize the formulation and technology of liposomes by single factor - orthogonal design. Results: The optimized formulation and preparation process were as follows: the hydration temperature was 55 ℃, the concentration of phospholipid was 3.5%, the ratio of phospholipid to cholesterol was 12:1, the ratio of lipid to drug was 15:1, and the mole percentage of DSPEMPEG2000 was 5%. Under this condition, the liposome encapsulation efficiency was 90.6%, the average particle size was 113.4 nm and the Zeta potential was -45.9 mV. CONCLUSION: The furanodiene long-circulating liposomes prepared in this study have high encapsulation efficiency, narrower particle size distribution and smaller average particle size, which has a good application prospect.