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

Research Project

Project/Area Number 21K06650
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47060:Clinical pharmacy-related
Research InstitutionJosai 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
Project Status Completed (Fiscal Year 2023)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2023: ¥260,000 (Direct Cost: ¥200,000、Indirect Cost: ¥60,000)
Fiscal Year 2022: ¥260,000 (Direct Cost: ¥200,000、Indirect Cost: ¥60,000)
Fiscal Year 2021: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
KeywordsAzone / イオン液体 / ante-enhancer / 皮膚透過 / 経皮吸収促進効果 / ionic liquid / skin permeation / Ionic Liquid / chemical enhancer / skin irritation
Outline of Research at the Start

皮膚は、ウイルスや薬物の体内への侵入を防ぐ機能があり、皮膚透過する有効性薬物の性質は限られてくる。これまで皮膚透過しにくいために、皮膚適用製剤にならなかった薬物は数多くある。1980年代に、皮膚透過促進効果が高い物質が開発された皮膚刺激性により、製品化にならなかった。そこで本研究では、低刺激性で皮膚透過促進効果が得られる物質を構築し、製剤化が可能であるか検討する。

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.

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。

Report

(3 results)
  • 2023 Annual Research Report   Final Research Report ( PDF )
  • 2022 Research-status Report
  • Research Products

    (4 results)

All 2024 2023

All Journal Article (2 results) (of which Peer Reviewed: 1 results) Presentation (2 results)

  • [Journal Article] Design of Ionic Liquid Formulations with Azone-Mimic Structures for Enhanced Drug Skin Permeation2024

    • Author(s)
      Oshizaka Takeshi、Yamamoto Aki、Tanaka Hikaru、Takeuchi Issei、Mori Kenji、Sugibayashi Kenji
    • Journal Title

      Journal of Pharmaceutical Sciences

      Volume: 113 Issue: 5 Pages: 1299-1305

    • DOI

      10.1016/j.xphs.2023.12.007

    • Related Report
      2023 Annual Research Report
  • [Journal Article] Design of an Ante-enhancer with an Azone-Mimic Structure using Ionic Liquid2023

    • Author(s)
      Oshizaka Takeshi、Hayakawa Mao、Uesaka Mayu、Yoshizawa Kota、Kamei Tomoyo、Takeuchi Issei、Mori Kenji、Itakura Shoko、Todo Hiroaki、Sugibayashi Kenji
    • Journal Title

      Pharmaceutical Research

      Volume: 未 Issue: 6 Pages: 1577-1586

    • DOI

      10.1007/s11095-023-03515-y

    • Related Report
      2022 Research-status Report
    • Peer Reviewed
  • [Presentation] Azone模倣構造を有するイオン液体型アンテエンハンサーを含む適切な製剤の選択2023

    • Author(s)
      山本 亜季、田中 光、押坂 勇志、竹内 一成、  森 健二、杉林 堅次
    • Organizer
      日本薬学会 第144年会
    • Related Report
      2023 Annual Research Report
  • [Presentation] イオン液体型ante-enhancerの薬物経皮吸収促進効果2023

    • Author(s)
      上坂 真由
    • Organizer
      日本薬学会 第143年会
    • Related Report
      2022 Research-status Report

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Published: 2021-04-28   Modified: 2025-01-30  

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