摘要
旨在提高二氢杨梅素(DMY)的生物利用度,制备了二氢杨梅素自微乳(DMY-SMES),通过DMY在辅料(油相、乳化剂和助乳化剂)中的溶解度及各辅料的相容性确定油相、乳化剂和助乳化剂,通过伪三元相图确定三者在自微乳中的比例,在此基础上,以粒径、多分散指数(PDI)和载药量为指标,通过单纯形网格法优化DMY-SMES的配方,并对最佳配方制备的DMY-SMES进行表征。结果表明:以中链甘油三酯(MCT)、吐温80和聚乙二醇400分别为油相、乳化剂和助乳化剂,DMY-SMES的最佳配方为10%MCT、60%吐温80、30%聚乙二醇400,在此条件下DMY-SMES的液滴平均粒径为14.46 nm,PDI为0.138,载药量为29.84 mg/g,包封率可达85.26%;最佳配方所得DMY-SMES为浅黄色澄清液体,乳滴呈类球形、粒径小、表面光滑,无团聚现象,为O/W型,自微乳及其稀释液的稳定性均较优;DMY-SMES的浊点为70℃;DMY-SMES在水、pH 1.2 HCl、pH 6.8磷酸盐缓冲液(PBS)中及在30 d的储藏期内(4℃),其液滴粒径和分布均无明显变化;DMY-SMES在水、pH 1.2 HCl、pH 6.8 PBS中的释放量明显高于游离DMY;在一定质量浓度下,DMY-SMES的DPPH和ABTS自由基清除能力强于游离DMY。综上,自微乳可提高DMY的溶解度,使其具有良好的生物相容性和稳定性,在食品工业和医药领域具有广阔的发展前景。
In order to improve the bioavailability of dihydromyricetin(DMY),dihydromyricetin self-microemulsifying system(DMY-SMES)was prepared.The solubility of DMY in excipients(oil phase,emulsifier,and co-emulsifier)and the compatibility of each excipient were investigated to determine the oil phase,emulsifier,and co-emulsifier.The proportions of these components in the self-microemulsifying system were determined based on the pseudo-ternary phase diagram.Then,the formulation of DMY-SMES was optimized by the simplex lattice method using particle size,polydispersity index(PDI)and drug loading as indicators.The DMY-SMES prepared with the optimal formulation was characterized.The results showed that with medium-chain triglycerides(MCT),Tween-80,and polyethylene glycol 400 as oil phase,emulsifier and co-emulsifier,respectively,the optimal formulation of DMY-SMES was 10%MCT,60%Tween-80,and 30%polyethylene glycol 400.Under these conditions,the average particle size of DMY-SMES was 14.46 nm,the PDI was 0.138,and the drug loading was 29.84 mg/g,with an encapsulation efficiency of 85.26%.The DMY-SMES obtained from the optimal formulation was a light yellow,clear liquid with spherical-like droplets,small particle size,smooth surface,and no aggregation,forming an O/W type.Both the self-microemulsifying system and its diluted solutions exhibited excellent stability.The cloud point of DMY-SMES was 70℃.The particle size and distribution of DMY-SMES in water,pH 1.2 HCl,and pH 6.8 phosphate buffer solution(PBS)showed no significant changes during the 30 d storage period(4℃).The release amount of DMY-SMES in water,pH 1.2 HCl,and pH 6.8 PBS was significantly higher than that of free DMY.At a certain mass concentration,the DPPH and ABTS free radical scavenging abilities of DMY-SMES were stronger than those of free DMY.In conclusion,the self-microemulsion system can improve the solubility of DMY,giving DMY good biocompatibility and stability,and it has broad prospects for development in the food industry and pharmaceutical field.
作者
常大伟
曹佳怡
姚芊
任娜
王虎玄
孙玉姣
沈文
CHANG Dawei;CAO Jiayi;YAO Qian;REN Na;WANG Huxuan;SUN Yujiao;SHEN Wen(College of Food Science and Engineering,Shaanxi University of Science&Technology,Xi′an 710021,China)
出处
《中国油脂》
北大核心
2025年第5期75-84,共10页
China Oils and Fats
基金
国家自然科学基金项目(32272446)
陕西省科技厅重点研发计划项目(2022NY-223)
陕西省西安市科技局农业技术研发计划项目(21NYYF0058)
陕西省重点研发计划项目(2023-YBSF-379)。
关键词
二氢杨梅素
自微乳
单纯形网格法
体外释放
dihydromyricetin
self-microemulsion
simplex lattice method
in vitro release
作者简介
常大伟(1978),男,副教授,博士,研究方向为功能因子的微胶囊、果蔬加工以及功能性配料与添加剂,(E-mail)cdw1860@126.com。
