The Enhanced Skin Permeation of Flavonoids Via the Application of a Coamorphous in a Microemulsion Formulation

微乳液 渗透 化学 溶解度 水溶液 色谱法 生物利用度 过饱和度 有机化学 肺表面活性物质 生物信息学 生物化学 生物
作者
Hiromasa Uchiyama,Yuka Hanamoto,Yuta Hatanaka,Kazunori Kadota,Yuichi Tozuka
出处
期刊:Journal of Pharmaceutical Sciences [Elsevier BV]
卷期号:112 (12): 3067-3074 被引量:2
标识
DOI:10.1016/j.xphs.2023.06.011
摘要

Improving the permeability and solubility of poorly water-soluble compounds is a major difficulty in skin permeation. In this study, we investigated whether using a pharmaceutical technique such as applying coamorphous to a microemulsion enhances the skin permeation of polyphenolic compounds. The melt-quenching technique created the coamorphous system between naringenin (NRG) and hesperetin (HPT), two polyphenolic compounds with poor water solubility. By creating a supersaturated state, the aqueous solution of coamorphous NRG/HPT demonstrated improved NRG and HPT skin permeation. However, as both compounds precipitated, the supersaturation ratio decreased. In contrast to crystal compounds, incorporating coamorphous material into microemulsions enabled the preparation of microemulsions in a wider formulation range. Additionally, compared to microemulsions with crystal compounds and an aqueous suspension of coamorphous, microemulsions with coamorphous NRG/HPT increased skin permeation of both compounds by more than four times. These results suggested that interactions between NRG and HPT are maintained in the microemulsion and enhance both compounds' skin permeation. An approach for improving the skin permeation of poorly water-soluble chemicals would be to apply a coamorphous system to a microemulsion.
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