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Hybrid formulations of the organic nanocomposite via structural investigations

Research Project

Project/Area Number 18K06614
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 InstitutionOsaka 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
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2020: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsナノコンポジット / 可溶化 / 複合体形成 / 処方設計 / ナノ集合体 / 溶解度改善 / 糖転移ステビア / 糖転移ナリンジン / 粉砕補助剤 / 糖転移ルチン / 糖転移へスぺリジン / 難水溶性化合物
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.

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。

Report

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

    (21 results)

All 2020 2019 2018

All Journal Article (7 results) (of which Peer Reviewed: 7 results) Presentation (14 results) (of which Int'l Joint Research: 3 results,  Invited: 2 results)

  • [Journal Article] Mixed micelles of the drug diphenhydramine hydrochloride with anionic and non-ionic surfactants show improve solubility, drug release and cytotoxicity of ethenzamide2019

    • Author(s)
      A. Srivastava, H. Uchiyama, Y. Wada, Y. Hatanaka, Y. Shirakawa, K. Kadota, Y. Tozuka
    • Journal Title

      J. Mol. Liq.

      Volume: 277 Pages: 349-359

    • DOI

      10.1016/j.molliq.2018.12.070

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] Enhanced solubility and permeability of quercetin by composite formation between α-glucosyl stevia and hydrophilic polymer2019

    • Author(s)
      H. Uchiyama, Y. Wada, Y. Hatanaka, Y. Hirata, M. Taniguchi, A. Nakanishi, M. Tandia, K. Kadota, Y. Tozuka
    • Journal Title

      J. Pharm. Sci.

      Volume: 108 Issue: 6 Pages: 2033-2040

    • DOI

      10.1016/j.xphs.2019.01.007

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] A simple blending with α-glycosylated naringin produce the enhancement of solubility and absorption of pranlukast hemihydrate2019

    • Author(s)
      H. Uchiyama, K. Kadota, A. Nakanishi, M. Tandia, Y. Tozuka
    • Journal Title

      Int. J. Pharm.

      Volume: 567 Pages: 118490-118490

    • DOI

      10.1016/j.ijpharm.2019.118490

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] Improved water dispersibility and photostability in folic acid nanoparticles with transglycosylated naringin using combined processes of wet-milling and freeze-drying2019

    • Author(s)
      K. Semba, K. Kadota, H. Arima, A. Nakanishi, M. Tandia, H. Uchiyama, K. Sugiyama, Y. Tozuka
    • Journal Title

      Food Res. Int.

      Volume: 121 Pages: 108-116

    • DOI

      10.1016/j.foodres.2019.03.034

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] Investigation of physiological properties of transglycosylated stevia with cationic surfactant and its application to enhance the solubility of rebamipide2018

    • Author(s)
      H. Uchiyama, A. Srivastava, M. Fujimori, K. Tomoo, A. Nakanishi, M. Tandia, K. Kadota, Y. Tozuka
    • Journal Title

      J. Phys. Chem. B

      Volume: 122 Issue: 43 Pages: 10051-10061

    • DOI

      10.1021/acs.jpcb.8b07515

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Journal Article] Emergent composite structures following the amorphization of itraconazole with transglycosylated rutin by over-grinding2018

    • Author(s)
      K. Kadota, H. Arima, R. Shakudo, K. Semba, H. Uchiyama, K. Sugiyama, Y. Tozuka
    • Journal Title

      Powder Technol

      Volume: 323 Pages: 69-75

    • DOI

      10.1016/j.powtec.2017.10.002

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Journal Article] Jelly containing composite based on α-glucosyl stevia and polyvinylpyrrolidone: Improved dissolution property of curcumin2018

    • Author(s)
      H. Uchiyama, S. Nogami, K. Katayama, K. Hayashi, K. Kadota, Y. Tozuka
    • Journal Title

      Euro. J. Pharm.Sci

      Volume: 117 Pages: 48-54

    • DOI

      10.1016/j.ejps.2018.02.011

    • Related Report
      2018 Research-status Report
    • Peer Reviewed
  • [Presentation] 機能性食品中に含有される難水溶性有効成分の可溶化技術:薬学研究の視点からの戦略2020

    • Author(s)
      戸塚裕一
    • Organizer
      第11回岐阜薬科大学機能性健康食品研究講演会
    • Related Report
      2020 Annual Research Report
    • Invited
  • [Presentation] 分子間相互作用に基づく機能性粒子・ナノ集合体の調製と医薬品・食品産業への新規処方の提案2020

    • Author(s)
      戸塚裕一
    • Organizer
      令和2年度第2回メディショナルナノテク研究会
    • Related Report
      2020 Annual Research Report
    • Invited
  • [Presentation] α-Glucosyl Steviaを用いた混合ミセル形成による小腸環境下でのClotrimazoleの溶解性改善2019

    • Author(s)
      木戸貴也、内山博雅、Anirudh Srivastava、門田和紀、戸塚裕一
    • Organizer
      日本薬剤学会第34年会
    • Related Report
      2019 Research-status Report
  • [Presentation] 経口ゼリー剤のテクスチャに及ぼす添加塩の影響2019

    • Author(s)
      野上聡、内山博雅、門田和紀、戸塚裕一
    • Organizer
      日本海水学会第70年会
    • Related Report
      2019 Research-status Report
  • [Presentation] 機能性食品開発を指向した湿式粉砕によるSilybinナノ粒子の調製2019

    • Author(s)
      藤森美季、内山博雅、門田和紀、戸塚裕一
    • Organizer
      製剤機械技術学会第29回大会
    • Related Report
      2019 Research-status Report
  • [Presentation] クルクミンゼリー剤の放出挙動に及ぼすテクスチャの影響2019

    • Author(s)
      野上聡、内山博雅、門田和紀、戸塚裕一
    • Organizer
      日本薬学会139年会
    • Related Report
      2018 Research-status Report
  • [Presentation] Investigation of mixed micelle formation between transglycosylated stevia and cationic surfactants with different carbon chain length2018

    • Author(s)
      M. Fujimori, H. Uchiyama, K. Kadota, Y. Tozuka
    • Organizer
      The 6th International Conference on the Characterization and Control of Interfaces (ICCCI2018) for High Quality Advanced Materials
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research
  • [Presentation] Preparation of jelly formulation with nano-composites structure containing curcumin2018

    • Author(s)
      S. Nogami, H. Uchiyama, K. Hayashi, K. Kadota, Y. Tozuka
    • Organizer
      The 2nd Workshop for Japan-Korea Young Scientists on Pharmaceutics
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research
  • [Presentation] A novel hybrid-nanocomposite formed by α-glucosyl stevia and water-soluble polymer: For dissolution enhancement of poorly soluble drugs2018

    • Author(s)
      H. Uchiyama, K. Hayashi, K. Kadota, Y. Tozuka
    • Organizer
      the 23rd International Congress of Chemical and Process Engineering (CHISA)
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research
  • [Presentation] 酵素処理イソクエルシトリンによる難溶解性フラボノイドの溶解性改善2018

    • Author(s)
      内山博雅、田中舜、門田和紀、箕浦克彦、戸塚裕一
    • Organizer
      日本食品化学学会第24回学術大会
    • Related Report
      2018 Research-status Report
  • [Presentation] 固体NMRによるcarbamazepine/α-glucosyl rutin非晶質固体分散体中の分子間相互作用の評価2018

    • Author(s)
      東顕二郎、青木千咲、石塚優也、植田圭祐、門田和紀、戸塚裕一、森部久仁一
    • Organizer
      日本薬剤学会第33年会
    • Related Report
      2018 Research-status Report
  • [Presentation] 糖転移ステビアとポリビニルピロリドンのコンポジット形成によるケルセチンの溶解性改善2018

    • Author(s)
      内山博雅、林圭太、門田和紀、戸塚裕一
    • Organizer
      日本薬剤学会第33年会
    • Related Report
      2018 Research-status Report
  • [Presentation] 小角X線散乱法による葉酸ナノ製剤の再分散性と構造評価2018

    • Author(s)
      仙波久実、有馬寛、内山博雅、門田和紀、杉山和正、戸塚裕一
    • Organizer
      日本薬剤学会第33年会
    • Related Report
      2018 Research-status Report
  • [Presentation] 混合ミセル構造と難溶性薬物の溶解性改善効果の検討2018

    • Author(s)
      佐藤公紀、藤森美季、Srivastava Anirudh、内山博雅、門田和紀、戸塚裕一
    • Organizer
      第68回日本薬学会近畿支部大会
    • Related Report
      2018 Research-status Report

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

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