【摘要】 目的:采用薄膜水化法制备包载雷公藤甲素的普朗尼克F127/F68混合胶束.方法:对制备方法中的可变因素,以及水化温度与药物泄漏相关性进行考察,在考虑混合胶束稳定的前提下优化制备工艺,提高载药量和包封率.结果:载药胶束的载药量和包封率与投药量、加水量以及水化温度均有关,当加水量达到一定时与普朗尼克F127和F68的质量比无关,并且水化温度越高越易导致胶束提早释药.按照载体材料F127/F68(1:1)200 mg,加水量20 m L,水化温度50℃的制备工艺制备载药胶束,可得到载药量和包封率分别为3.47%和90.09%.结论:制备的雷公藤甲素普朗尼克混合载药胶束的制备方法简单,虽然载药量较低,但适合作为低剂量抗癌药物雷公藤甲素的载体.实验结果将为进一步研究雷公藤甲素的多功能载体打下基础.更多还原

【Abstract】 Objective:To prepare Pluronic F127/F68 mixed micelles containing triptolide(TPL)by the film-hydration method. Methods:The variable factors in the preparation method and the correlation between hydration temperature and drug leakage were investigated. Under the premise of considering the stability of the mixed micelles,the preparation process was optimized to improve drug-loading amount and encapsulation rate. Results:The drug loading amount and encapsulation rate were related to the dosage of TPL,water quantity and hydration temperature,but not to the mass ratio of Pluronic F127 and F68 when water quantity reaches a certain level,and the higher the hydration temperature is,the more likely the micelle was to release early. According to the optimized preparation process:carrier material F127/F68(1:1)was 200 mg,water volume was 20 mL,hydration temperature was 50℃,to prepare drug-loaded micelles,the drug-loaded capacity and encapsulation rate were 3.47% and 90.09% respectively. Conclusion:The preparation method of triptolide-loaded Pluronic mixed micelles is simple. Although the drug loading is low,it is suitable as a carrier for the low-dose anticancer drug triptolide. The experimental results will lay the foundation for further research on the multifunctional carrier of triptolide.更多还原