二氢卟吩e6磁性声敏纳米脂质体的制备及质量评价

发布时间：2019-06-28 13:04

【摘要】：目的:优选二氢卟吩e6(Ce6)磁性声敏纳米脂质体的处方及制备工艺,建立其质量评价方法。方法:采用薄膜分散-真空冷冻干燥技术制备Ce6磁性声敏纳米脂质体,以包封率为指标,通过正交试验考察有机相种类、水化介质、水化温度、水化时间对脂质体制备工艺的影响,考察卵磷脂与胆固醇的质量比、药脂比、药磁比、聚山梨酯-80(tween-80)用量对脂质体处方工艺的影响。采用透射电镜观察其形态,粒度测量仪测定其粒径,动态透析法考察其体外释放的声敏特性并与普通脂质体进行比较。结果:最佳制备工艺条件为有机相三氯甲烷,水化介质水,水化时间50 min,水化温度55℃;最佳配方为药脂比1∶50,卵磷脂-胆固醇(5∶1),tween-80用量0.5%,药磁比1∶2。制备的Ce6磁性声敏纳米脂质体透射电镜下呈球形粒子分布,其外观圆整、大小均一,平均包封率90.28%,渗漏率3.28%,粒径176.9 nm。随着超声时间(0~150 s)和超声强度(0~2.0 W·cm-2)的增加,Ce6磁性声敏纳米脂质体的体外累积释放度增大。结论:采用薄膜分散-真空冷冻干燥法制备的Ce6磁性声敏纳米脂质体粒径均匀、包封率高,具有良好的体外声敏特性。
[Abstract]:Objective: to optimize the formulation and preparation process of dihydroporphine e6 (Ce6) magnetic sound sensitive nanoliposomes and to establish a quality evaluation method. Methods: Ce6 magnetic sound sensitive nanoliposomes were prepared by thin film dispersion vacuum freeze drying technique. The effects of organic phase type, hydration medium, hydration temperature and hydration time on the preparation process of liposomes were investigated by orthogonal test. The effects of the mass ratio of lecithin to cholesterol, the ratio of drug to lipid, the ratio of drug to magnetic and the dosage of polysorbate 80 (tween-80) on the formulation of liposomes were investigated. Its morphology was observed by transmission electron microscope, its particle size was measured by particle size measuring instrument, and the sound sensitivity of its release in vitro was investigated by dynamic dialysis method and compared with that of ordinary liposomes. Results: the optimum preparation conditions were as follows: organic phase trichloromethane, hydration medium water, hydration time 50 min, hydration temperature 55 鈩，

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