二氢杨梅素自微乳配方的优化及表征Formulation optimization and characterization of self-microemulsifying system for dihydromyricetin

• Published in: Zhongguo you zhi Vol. 50; no. 5; pp. 75 - 84
• Main Author: 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
• Format: Journal Article
• Language: English
• Published: 中粮工科（西安）国际工程有限公司 01.05.2025
• Subjects: dihydromyricetin; self-microemulsion; simplex lattice method; in vitro release; 二氢杨梅素；自微乳；单纯形网格法；体外释放
• ISSN: 1003-7969
• DOI: 10.19902/j.cnki.zgyz.1003-7969.240080

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.