【摘要】：目的:優(yōu)選二氫卟吩e6(Ce6)磁性聲敏納米脂質(zhì)體的處方及制備工藝,建立其質(zhì)量評價方法。方法:采用薄膜分散-真空冷凍干燥技術(shù)制備Ce6磁性聲敏納米脂質(zhì)體,以包封率為指標(biāo),通過正交試驗考察有機(jī)相種類、水化介質(zhì)、水化溫度、水化時間對脂質(zhì)體制備工藝的影響,考察卵磷脂與膽固醇的質(zhì)量比、藥脂比、藥磁比、聚山梨酯-80(tween-80)用量對脂質(zhì)體處方工藝的影響。采用透射電鏡觀察其形態(tài),粒度測量儀測定其粒徑,動態(tài)透析法考察其體外釋放的聲敏特性并與普通脂質(zhì)體進(jìn)行比較。結(jié)果:最佳制備工藝條件為有機(jī)相三氯甲烷,水化介質(zhì)水,水化時間50 min,水化溫度55℃;最佳配方為藥脂比1∶50,卵磷脂-膽固醇(5∶1),tween-80用量0.5%,藥磁比1∶2。制備的Ce6磁性聲敏納米脂質(zhì)體透射電鏡下呈球形粒子分布,其外觀圓整、大小均一,平均包封率90.28%,滲漏率3.28%,粒徑176.9 nm。隨著超聲時間(0~150 s)和超聲強(qiáng)度(0~2.0 W·cm-2)的增加,Ce6磁性聲敏納米脂質(zhì)體的體外累積釋放度增大。結(jié)論:采用薄膜分散-真空冷凍干燥法制備的Ce6磁性聲敏納米脂質(zhì)體粒徑均勻、包封率高,具有良好的體外聲敏特性。
[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，

本文編號：2507324