论文部分内容阅读
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。
Objective: To optimize the preparation and preparation of chlorin e6 (Ce6) magnetically sensitized nanoliposomes and to establish the quality evaluation method. Methods: Ce6 magnetically sensitized nanoliposomes were prepared by thin-film dispersion-vacuum freeze-drying technique. The encapsulation efficiency was used as an index to study the effect of organic phase, hydration medium, hydration temperature and hydration time on lipid The effects of lecithin and cholesterol mass ratio, drug-lipid ratio, drug-magnetic ratio, and the amount of tween-80 on liposome preparation were investigated. The morphology was observed by transmission electron microscopy. The particle size was measured by particle size analyzer. The dynamic properties of dialysis were investigated by dynamic dialysis and compared with the normal liposomes. Results: The optimal preparation conditions were as follows: organic phase chloroform, hydration medium water, hydration time 50 min, hydration temperature 55 ℃. The optimal formula was 1:50 for ratio of lipid to lipid, 5: 1 for lecithin-cholesterol ), tween-80 dosage 0.5%, magnetic ratio 1: 2. The prepared Ce6 magnetically sensitized nanoliposomes showed spherical particle distribution under transmission electron microscope and the appearance was round and uniform in size with an average encapsulation efficiency of 90.28%, a leakage rate of 3.28% and a particle size of 176.9 nm. With the increase of ultrasonic time (0 ~ 150 s) and ultrasonic intensity (0 ~ 2.0 W · cm-2), the cumulative release of Ce6 magnetically sensitized nanoliposomes increased in vitro. CONCLUSION: Ce6 magnetic nanosensitive nanosized liposomes prepared by membrane dispersion-vacuum freeze-drying method have uniform particle size and high entrapment efficiency, and have good in vitro acoustic sensitivities.