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机构地区:[1]沈阳药科大学,沈阳110016 [2]宁夏启元国药有限公司,银川750100
出 处:《中国新药杂志》2016年第21期2500-2505,共6页Chinese Journal of New Drugs
摘 要: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 long-circulation liposomes containing furanodiene.Methods: Liposomes were prepared by a thin-film ultrasonic dispersion method. With encapsulation efficiency and particle size as indexes,the formulation and preparation process was optimized by the single factor experiment and orthogonal test. Results: The optimized formulation was as follows: the hydration temperature was 55 ℃,the concentration of phospholipid was 3. 5%,weight ratio of phospholipid to cholesterol was 12 ∶ 1,weight ratio of phospholipid to drug was 15 ∶ 1,and molar ratio of DSPE-MPEG2000 was 5%. The encapsulation efficiency of furanodiene liposomes was 90. 6% with an average diameter of 113. 4 nm and the Zeta potential of-45. 9 m V.Conclusion: The prepared furanodiene liposomes have higher entrapment efficiency, and lower particle size distribution. And smaller particle size,showing a great potential for further investigation.
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