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

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K06595
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
• Research Institution: Okayama 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
• 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

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.

Free Research Field

薬剤学

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。