日用化学工业（中英文）2025，Vol.55Issue(4)：453-463,11.DOI:10.3969/j.issn.2097-2806.2025.04.007
氧化白藜芦醇自微乳的制备、表征及美白活性的研究
Preparation,characterization,and whitening activity research of oxyresveratrol-loaded self-microemulsion
摘要
Abstract
A self-microemulsifying drug delivery system(OXY-SME)was developed using Cremophor® EL and Labrasol® as composite emulsifiers to efficiently load oxyresveratrol(OXY),and its formulation characteristics,stability,in vitro skin permeation,and whitening activity were evaluated.Through the pseudo-ternary phase diagram and testing the particle size and polydispersity index(PDI)of the emulsion,the formulation for the preparation of blank self-microemulsion(SME)and the optimal drug loading of OXY were determined.At the optimal drug loading of 4%,the particle size of OXY-SME was(18.69±0.29)nm,with a PDI of 0.181±0.017 and an encapsulation efficiency of 99.87%±1.50%.The emulsion droplets were spherical,and the solubility of OXY in water was increased by approximately 62 times.The relationship between emulsion type and water content of OXY-SME was clarified using water content-conductivity fitting curves and staining methods.The stability of OXY-SME under various conditions was evaluated by measuring particle size,PDI,and OXY content.The results indicate that OXY-SME exhibits good storage stability and dilution stability,and effectively delays the decrease in OXY content caused by light exposure.The effect of water content on OXY skin permeation was investigated using the abdominal skin of SD rats,and the results show that the highest cumulative skin permeation of OXY over 48 hours is observed at a water content of 70%,indicating an oil-in-water(O/W)type emulsion.The whitening activity of OXY-SME was evaluated by measuring the activity of mushroom tyrosinase and intracellular tyrosinase in B16-F10 cells,as well as melanin content.OXY-SME exhibits stronger inhibitory effects on intracellular tyrosinase activity and melanin production compared to OXY aqueous solution and kojic acid(KA)as a positive control,demonstrating that OXY-SME enhances intracellular whitening activity of OXY.关键词
氧化白藜芦醇/自微乳递送系统/溶解度/稳定性/体外皮肤渗透/美白活性Key words
oxyresveratrol/self-microemulsion delivery system/solubility/stability/in vitro skin penetration/whitening activity分类
化学化工引用本文复制引用
苗开元,欧阳泽垚,赵新颖,杨晓婧,陈欣妍,石召华..氧化白藜芦醇自微乳的制备、表征及美白活性的研究[J].日用化学工业（中英文）,2025,55(4):453-463,11.基金项目
湖北省重大科技专项项目(2024BCA002) （2024BCA002）
校级中医药重点专项(2022ZZXZ003) （2022ZZXZ003）
