Preparation of Essential Oil-Based Microemulsions for Improving the Solubility, pH Stability, Photostability, and Skin Permeation of Quercetin

微乳液 渗透 槲皮素 溶解度 化学 色谱法 水溶液 有机化学 肺表面活性物质 生物化学 抗氧化剂
作者
Xia Lv,Tiantian Liu,Huipeng Ma,Yan Tian,Lei Li,Zhen Li,Meng Gao,Jianbin Zhang,Lei Gao
出处
期刊:Aaps Pharmscitech [Springer Nature]
卷期号:18 (8): 3097-3104 被引量:54
标识
DOI:10.1208/s12249-017-0798-x
摘要

Quercetin can bring many benefits to skin based on its various bioactivities. However, the therapeutic effect of quercetin is limited due to the poor water solubility, pH instability, light instability, and skin permeation. The aim of the present work was applying essential oil-based microemulsions to improve the solubility, pH stability, photostability, and skin permeation of quercetin for topical application. Peppermint oil (PO-ME), clove oil (CO-ME), and rosemary oil (RMO-ME) were selected as model essential oils. Microemulsions composed of Cremophor EL/1,2-propanediol/essential oils (47:23:30, w/w) were selected as model formulations, based on the pseudo-ternary phase diagram and the characterizations. In the solubility study, the solubility of quercetin was improved dozens of times by microemulsions. Quercetin was found instable under alkaline condition, with 50% degraded in the solution of pH 13. However, PO-ME, CO-ME, and RMO-ME could protect quercetin from the hydroxide ions, with 47, 9, and 12% of quercetin degraded. In the photostability study, the essential oil-based microemulsions showed the capability of protecting quercetin from degradation under UV radiation. Where more than 67% of quercetin was degraded in aqueous solution, while less than 7% of quercetin degraded in microemulsions. At last, the in vitro skin permeation study showed that the essential oil-based microemulsions could enhance the permeation capacity of quercetin by 2.5–3 times compared to the aqueous solution. Hence, the prepared essential oil microemulsions could improve the solubility, pH stability, photostability, and skin permeation of quercetin, which will be beneficial for its topical application.

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