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Utilization of supersaturated dosage form and micro-puncture formation on skin to a new transdermal drug delivery

Research Project

Project/Area Number 18K06595
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
Research InstitutionOkayama University

Principal Investigator

Kurosaki Yuji  岡山大学, 医歯薬学総合研究科, 教授 (90161786)

Project Period (FY) 2018-04-01 – 2021-03-31
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2020: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2019: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2018: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Keywords過飽和形成製剤 / 固体分散体 / 経皮的薬物送達 / マイクロニードル / 角質層侵襲 / L-HPC / 含水ゲルシート / ナノファイバー / 薬物透過障壁 / 抗マラリア / N-251 / 抗マラリア薬 / 皮膚透過障壁 / L-HPC含水ゲルシート / 経皮適用型製剤
Outline of Final Research Achievements

A supersaturated preparation by forming a solid dispersion (SD) of a poorly water-soluble model drug and a water-soluble polymer was investigated. The disappearance of the endothermic peak due to SD conversion was confirmed by DSC. A supersaturated state was formed immediately after dissolution due to SD conversion, but a gradual decrease in solubility was observed.
In vitro skin permeation experiments confirmed a significant increase in the amount of drug transferred into the skin tissue due to the combined use of supersaturation-forming formulation and skin microneedle puncture of the skin. Furthermore, the amount of intradermal transfer was increased by dressing the skin surface to which the SD preparation was applied with a hydrogel sheet.

Academic Significance and Societal Importance of the Research Achievements

皮膚適用型医薬品は患者自身が投与できる製剤であり、医療環境に恵まれていない地域での医療を飛躍的に改善する可能性を有する。しかし、難溶性薬物の経皮的薬物送達において、(1) 薬物の溶解性の改善 と (2) 薬物の皮膚透過の促進 が医薬品開発上の最大の障壁となっている。
本研究では、難水溶性モデル薬物と水溶性高分子との固体分散体(SD)化による過飽和形成製剤の調製ならびに美容領域での使用実績のあるマイクロニードルによる皮膚穿刺を組合わせることにより、皮膚適用型医薬品の新たな設計・評価ストラテジーを示すことができた。

Report

(4 results)
  • 2020 Annual Research Report   Final Research Report ( PDF )
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (3 results)

All 2021 2020 2018

All Presentation (3 results) (of which Int'l Joint Research: 1 results)

  • [Presentation] 新しいマラリア治療薬の開発̶-軟膏製剤としての実用化に向けた基礎研究2021

    • Author(s)
      井黒香奈⼦、五十川怜奈、池田奈々子、黒崎勇二、Kyung-Soo Chang、金惠淑
    • Organizer
      日本薬学会第141年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] 新しいマラリア治療薬の開発̶-過酸化物をベースにした軟膏製剤の基礎研究2020

    • Author(s)
      井黒香奈⼦、五十川怜奈、池田奈々子、黒崎勇二、Kyung-Soo Chang、金惠淑
    • Organizer
      グローバルヘルス合同大会2020
    • Related Report
      2020 Annual Research Report
  • [Presentation] Dermal super-saturated delivery (DSSD) of antimalarial-endoperoxides: A new strategy for dosage form designing.2018

    • Author(s)
      Yuji Kurosaki, Keisuke Sasaoka, Rina Morikami and Nana Taira
    • Organizer
      14th International Congress of Parasitology (ICOPA 2018) , Daegu, Korea, 8.19-24, 2018.
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research

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Published: 2018-04-23   Modified: 2022-01-27  

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