Page 162 - 《精细化工》2022年第7期

第 39 卷第 7 期 精 细 化 工 Vol.39, No.7
2022 年 7 月 FINE CHEMICALS July 2022

医药与日化原料
包载槲皮素 P/O/W 多重 Pickering 乳液的制备及表征

杨佳慧 1,2 ，梁 蓉 1,2* ，杨 成 1,2

（1. 江南大学 合成与生物胶体教育部重点实验室，江苏 无锡 214122；2. 江南大学 化学与材料工程学
院，江苏 无锡 214122）

摘要：以疏水 SiO 2 （AEROSIL®R202）、亲水 SiO 2 （AEROSIL®200）为乳化剂，一缩二丙二醇和甘油为内醇相，
制备了水包油包醇（P/O/W）多重 Pickering 乳液，用其对槲皮素进行了包载。考察了内醇相质量分数、疏水 SiO 2
质量分数、水乳比、亲水 SiO 2 质量分数对 P/O/W 多重 Pickering 乳液性能的影响。采用激光扫描共聚焦显微镜
（CLSM）、XRD 对 P/O/W 多重乳液及包载槲皮素后的 P/O/W 多重乳液进行了表征。结果表明，P/O/W 多重
Pickering 乳液制备的最佳条件为：内醇相〔m(甘油)∶m(一缩二丙二醇)=6∶4〕质量分数为 20%、疏水 SiO 2 质
量分数为 3%、m(水相)∶m(P/O 初乳)=5∶5、亲水 SiO 2 质量分数为 2%。包载后槲皮素的结晶峰消失，表明该多
重乳液对槲皮素有良好的包载效果。离心法测得包载槲皮素 P/O/W 多重乳液的载药量达 0.45%±0.02%。体外透
皮实验和猪皮 CLSM 显示，槲皮素经该多重乳液包载后透皮性能得到改善，这主要归因于槲皮素在内醇相中的
溶解度可达(60.0±2.1) mg/g，远高于其在水（<0.5 μg/g）或油（<1 mg/g）中的溶解度。
关键词：槲皮素；P/O/W 多重 Pickering 乳液；溶解度；载药量；透皮性能；医药原料
中图分类号：TQ658；O648.2+3 文献标识码：A
文章编号：1003-5214 (2022) 07-1448-09 开放科学 (资源服务) 标识码 (OSID)：

Preparation and characterization of quercetin-loaded P/O/W
multiple Pickering emulsions

1,2
1,2
YANG Jiahui , LIANG Rong 1,2* , YANG Cheng
（1. Key Laboratory of Synthetic and Biological Colloids, Ministry of Education, Jiangnan University, Wuxi 214122,
Jiangsu, China; 2. School of Chemical and Material Engineering, Jiangnan University, Wuxi 214122, Jiangsu, China）

Abstract: Polyol-in-oil-in-water (P/O/W) multiple Pickering emulsions were prepared to encapsulate
quercetin using hydrophobic silica (AEROSIL®R202) and hydrophilic silica (AEROSIL®200) as
emulsifiers, dipropylene glycol and glycerol as polyol phase. The effects of mass fractions of internal polyol
phase, hydrophobic and hydrophilic silica as well as water to emulsion ratio on the encapsulation properties
of P/O/W multiple Pickering emulsion for quercetin were investigated. Then the P/O/W double emulsion
with/without quercetin loaded were characterized by confocal laser scanning microscope (CLSM) and XRD.
The results showed that the optimum preparation conditions were obtained when mass fractions of internal
alcohol phase [m(glycerol)∶m(dipropylene glycol)=6∶4], hydrophobic silica and hydrophilic silica
reached 20%, 3%, and 2% respectively while water to emulsion ratio m(aqueous phase)∶m(P/O primary
emulsion) was kept at 5∶5. The crystalline peak of quercetin, when encapsulated, could not be observed,
indicating multiple P/O/W emulsion with excellent encapsulation capacity. The drug loading efficiency of
the P/O/W emulsion for quercetin reached 0.45%±0.02% analyzed by HPLC after centrifugation. In vitro
transdermal experiment and pig skin CLSM analysis indicated that encapsulation enhanced the transdermal
performance of quercetin, which was mainly attributed to the fact that the solubility of quercetin in the internal
polyol phase increased up to (60.0±2.1) mg/g, much high than that in water (<0.5 μg/g) or in oil (<1 mg/g).

收稿日期：2021-12-30; 定用日期：2022-04-01; DOI: 10.13550/j.jxhg.20211336
基金项目：国家重点研发计划资助（2016YFD0400801）
作者简介：杨佳慧（1997—），女，硕士生，E-mail：yjhzz0828@163.com。联系人：梁 蓉（1983—），女，副教授，E-mail：rongliang@
jiangnan.edu.cn。