Solubilization of poorly water‐soluble bioactive molecules in neutral aqueous media by complexation with renatured β‐1,3‐1,6‐glucan nanoparticles

  • Ayumu Kodama
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan
  • Akifumi Nakagawa
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan
  • Yuki Nonoguchi
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan
  • Haruka Sakurai
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan
  • Chieko Yano
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan
  • Toshio Suzuki
    Department of Applied Chemistry and Bioengineering Graduate School of Engineering, Osaka City University Osaka Japan
  • Kazuya Koumoto
    Department of Nanobiochemistry, Faculty of Frontiers of Innovative Research in Science and Technology (FIRST) Konan University Kobe Japan

抄録

<jats:title>Abstract</jats:title><jats:p>The design of scaffolds for solubilizing/dispersing poorly water‐soluble bioactive molecules in neutral aqueous media is a major challenge of functional food, pharmaceuticals, and cosmetics development, as highlighted by the plethora of corresponding solubilization/dispersion strategies. Herein, renatured β‐1,3‐1,6‐glucan (r‐glucan) nanoparticles prepared by neutralization of alkali‐denatured β‐1,3‐1,6‐glucan and subsequent centrifugation are used as a host to disperse water‐insoluble bioactive molecules (curcumin, all‐<jats:italic>trans</jats:italic>‐retinoic acid, and rebamipide) by simple mixing of host and guest solutions. Curcumin in the r‐glucan cavity is found to be stacked in the form of <jats:italic>J</jats:italic>‐aggregates and twisted along the helix, and is demonstrated to be retained for significantly longer than curcumin in the corresponding γ‐cyclodextrin (γ‐CD) complex. Specifically, curcumin incorporated in γ‐CD is released within 5.5 hours, whereas that in the r‐glucan complex is released very slowly, with 12% of curcumin in the latter complex retained after 31‐day incubation at 37°C. Thus, inclusion protocol simplicity and slow release ability make r‐glucan nanoparticles a potential carrier scaffold for various applications.</jats:p>

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