烟台大学学报(自然科学与工程版)2025,Vol.38Issue(2):208-216,9.DOI:10.13951/j.cnki.37-1213/n.240201
星点设计-效应面法优化鼠尾草酸自微乳载药系统
Optimization of Carnosic Acid Self-microemulsion Drug Delivery System by Central Composite Design-Response Surface Methodology
摘要
Abstract
This study aimed to establish a carnosic acid self-microemulsion drug delivery system(CA-SMEDDS)to expand the clinical application of carnosic acid(CA).The formula for the self-microemulsion was preliminarily screened by saturation solubility and pseudo-ternary phase diagram and further optimized by central composite de-sign-response surface methodology.The preliminary stability,in vitro release,and oral bioavailability in rats of CA-SMEDDS were also evaluated.The mass fraction of each excipient in the optimal formulation of CA-SMEDDS was as follows:oil phase(ethyl oleate)23.16%,emulsifier(EL-35)54.44%,co-emulsifier(PEG400)22.40%.Preliminary stability experiments showed that CA-SMEDDS were stable at 4℃and 25℃under light-avoiding con-ditions,and in vitro release experiments showed that their release rate was significantly higher than that of CA in enzyme-free release medium of both simulated gastric and intestinal fluid.The results of the pharmacokinetic study in rats showed that,compared with the CA control group,the relative bioavailability of CA-SMEDDs increased by 0.86 times.The preparation process of CA-SMEDDS was stable,which can significantly improve the dissolution rate and increase the oral bioavailability of carnosic acid.关键词
鼠尾草酸/自微乳给药系统/星点设计/效应面法/体外释放/生物利用度Key words
carnosic acid/self-microemulsion drug delivery system/central composite design/response surface methodology/in vitro release/bioavailability分类
药学引用本文复制引用
张丽芬,李凌娜,李蓉,周小魏,何杰,李刚,王振华,马成俊..星点设计-效应面法优化鼠尾草酸自微乳载药系统[J].烟台大学学报(自然科学与工程版),2025,38(2):208-216,9.基金项目
山东省自然科学基金资助项目(ZR2020MH380) (ZR2020MH380)
烟台市科技创新发展计划项目(2021XDHZ078). (2021XDHZ078)