姜黄素自乳化释药系统Caco-2细胞模型的建立

发布时间：2018-07-05 04:04

本文选题：SEDDS + 最优处方　；参考：《南昌大学》2017年硕士论文

【摘要】：本文以控制变量法筛选对姜黄素中CurI和CurII2个成分溶解性均较好的辅料,采用D-optimal混料设计,以上述2个成分的载药量、粒径和乳化时间为指标,对姜黄素自乳化释药系统进行处方优化,并进行初步质量评价。得出的姜黄素SEDDS最优处方为:Tween-20-Obleique CC497-Transcutol P=0.49:0.17:0.33(m:m:m),与原料药相比较,该处方在水中的溶解度分别增大了80和209倍,乳化时间9.1 s,平均粒径186 nm。且CurI和CurII 2个成分在溶出介质中溶出率高、溶出速度快,45min内累积溶出率已达95%以上,而原料药中这2种成分几乎不溶,原料药和含药SEDDS均有较好的油水分配系数,logP=2~3,预测姜黄素SEDDS为易吸收药物。在此基础上建立了Caco-2细胞模型,对Caco-2细胞单层完整性进行了考察。并采用CCK-8法考察了Cur SEDDS的细胞毒性对Caco-2单层细胞模型的影响及Cur SEDDS对Caco-2单层细胞模型TEER值的影响。
[Abstract]:In this paper, the excipients with good solubility of Curi and CurII in curcumin were screened by controlling variable method. D-optimal mixture design was used. The drug loading, particle size and emulsifying time of the two components were taken as indexes. The prescription of curcumin self-emulsifying drug release system was optimized and its quality was evaluated. The optimum formulation of curcumin SEDDS is: Tween-20-Obleique CC497-Transcutol 0.49: 0.17: 0.33 (m:m). The solubility of the prescription in water is increased by 80 and 209 times, the emulsification time is 9.1 s, and the average particle size is 186 nm compared with the raw drug. Moreover, the dissolution rate of Curi and CurII was high in dissolution medium. The cumulative dissolution rate of Curi and CurII in 45 minutes was over 95%, but the two components were almost insoluble. The oil and water partition coefficients of crude drug and drug containing SEDDS were better than that of control group, and curcumin SEDDS was predicted to be an easily absorbable drug. A Caco-2 cell model was established and the monolayer integrity of Caco-2 cells was investigated. The effects of cytotoxicity of cur-SEDDS on Caco-2 monolayer cell model and the effect of cu-SEDDS on TEER value of Caco-2 monolayer cell model were investigated by CCK-8 method.
【学位授予单位】：南昌大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：R943

【参考文献】