Design of an Ante‑enhancer with an Azone‑Mimic Structure and skin permeation enhancing effect of drug using Ionic Liquid

2023 Fiscal Year Final Research Report

• Project/Area Number: 21K06650
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47060:Clinical pharmacy-related
• Research Institution: Josai International University
• Principal Investigator: Oshizaka Takeshi 城西国際大学, 薬学部, 准教授 (80884030)
• Co-Investigator(Kenkyū-buntansha): 森 健二 城西国際大学, 薬学部, 教授 (60439023) ; 武井 千弥 城西国際大学, 薬学部, 助教 (70838466)
• Project Period (FY): 2021-04-01 – 2024-03-31
• Keywords: Azone / イオン液体 / ante-enhancer / 皮膚透過 / 経皮吸収促進効果

Outline of Final Research Achievements

In this study, we considered designing Azone-mimic structure ante-enhancers (additives that degrade after showing effect but before side effects). Ionic liquid (IL) preparation method was used to design the ante-enhancers. the reagents used for the design of the ante-enhancers were, ε-caprolactam and myristic acid. It was possible to prepare an IL form of Azone (IL-Azone) from ε-caprolactam and myristic acid. The IL-Azone prepared in this study had a skin permeation enhancing effect and reduced skin irritation compared to Azone. The best base material for IL-Azone was white petrolatum, which showed higher skin permeation enhancement effect than Azone when applied to the skin at the same time as the active ingredient.

Free Research Field

薬学

Academic Significance and Societal Importance of the Research Achievements

本研究では、イオン液体技術に着目して、Azone構造類似のイオン液体型アンテエンハンサーを設計することで、経皮吸収促進効果があり、かつAzoneよりも低刺激性の経皮吸収促進剤を設計することができた。この結果は、Azoneだけでなく、その他の経皮吸収促進剤についても、イオン液体型アンテエンハンサーの設計の可能性があり、より安全な製剤の開発を可能にすると示唆された。