Hybrid formulations of the organic nanocomposite via structural investigations

2020 Fiscal Year Final Research Report

• Project/Area Number: 18K06614
• 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: Osaka University of Pharmaceutical Sciences
• Principal Investigator: Tozuka Yuichi 大阪薬科大学, 薬学部, 教授 (50312963)
• Project Period (FY): 2018-04-01 – 2021-03-31
• Keywords: ナノコンポジット / 可溶化 / 複合体形成 / 処方設計

Outline of Final Research Achievements

There are many poorly water-soluble substances in pharmaceutical and health food products. Recently, we have reported the feasibility of transglycosylated food additives as novel pharmaceutical excipients to improve the dissolution and bioavailability of poorly water-soluble drugs. We reported in the present study that transglycosylated food additives self-associated into small micelles with a core-shell like architecture, in which the hydrophobic skeleton is segregated from the aqueous exterior to form a novel drug-loading core surrounded by a hydrophilic shell of sugar groups. The detailed structure of associated structure was differed among four types of transglycosylated food additives. We found that the usefulness of a novel hybrid composite formation together with transglycosylated food additive and hydrophilic polymer, resulting in the dramatical enhancement of the solubility and membrane permeability of hydrophobic substances.

Free Research Field

製剤学

Academic Significance and Societal Importance of the Research Achievements

すでに市販され、機能性食品などに幅広く用いられている食品添加剤を従来のコンセプトにはない手法で使用して、水に溶けにくい化合物を劇的に溶解させ、吸収を高めるような、「ナノコンポジット構造を持った可溶化構造体」の作成および構造の推定に成功した。また本研究では、汎用されている高分子素材と組み合わせて、より安定なナノコンポジット構造を作ることにも成功し、その構造を維持させたままでゼリー化することにも成功した。本成果が、医薬品・食品産業で水に溶けなくて利用が難しい化合物を溶けやすくしたり、ゼリー化して有効活用するための一助になることが期待される。