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<p>This study evaluates the in vivo mucoadhesive properties of thiolated cyclodextrins (CDs) with varying S-protection using polyethylene glycol (PEG) of different chain lengths. Free thiol groups of thiolated β-CDs (CD-SH) were S-protected with 1&#xa0;kDa and 2&#xa0;kDa PEG bearing a terminal thiol group, leading to third-generation of thiolated CDs (CD-SS-PEG). The structure of these thiolated CDs was confirmed and characterized by FT-IR, 1&#xa0;H NMR, and colorimetric assays. Thiolated and S-protected CDs were evaluated regarding viscosity, cellular uptake and, in vitro and in vivo mucoadhesion. The viscosity of CD-SH, CD-SS-PEG 1&#xa0;kDa, and CD-SS-PEG 2&#xa0;kDa mixtures with mucus increased 9-, 7-, and 5.5-fold, respectively, compared to unmodified CD within 3&#xa0;h. Cellular uptake on Caco-2 cells was 1.75 times higher for highly thiolated CDs than for unmodified CD. In vitro residence time on porcine intestine was prolonged 7-, 8.4-, and 7.9-fold for CD-SH, CD-SS-PEG 1&#xa0;kDa, and CD-SS-PEG 2&#xa0;kDa, respectively. In vivo results indicated CD-SS-PEG 1&#xa0;kDa had the highest potential. Our comprehensive in vitro, ex vivo, and in vivo ffindings demonstrate that CD-SS-PEG 1&#xa0;kDa is a highly promising candidate for mucoadhesive drug delivery systems.</p> Graphical Abstract <p></p>

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Cyclodextrin-mediated enhancement of gastrointestinal drug delivery: unveiling mucoadhesive and mucopenetrating synergy

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年3月20日

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  • Soheil Haddadzadegan,
  • Ahmad Saleh,
  • Florina Veider,
  • Patrick Knoll,
  • Flavia Laffleur,
  • Gergely Kali,
  • Andreas Bernkop-Schnürch

摘要

This study evaluates the in vivo mucoadhesive properties of thiolated cyclodextrins (CDs) with varying S-protection using polyethylene glycol (PEG) of different chain lengths. Free thiol groups of thiolated β-CDs (CD-SH) were S-protected with 1 kDa and 2 kDa PEG bearing a terminal thiol group, leading to third-generation of thiolated CDs (CD-SS-PEG). The structure of these thiolated CDs was confirmed and characterized by FT-IR, 1 H NMR, and colorimetric assays. Thiolated and S-protected CDs were evaluated regarding viscosity, cellular uptake and, in vitro and in vivo mucoadhesion. The viscosity of CD-SH, CD-SS-PEG 1 kDa, and CD-SS-PEG 2 kDa mixtures with mucus increased 9-, 7-, and 5.5-fold, respectively, compared to unmodified CD within 3 h. Cellular uptake on Caco-2 cells was 1.75 times higher for highly thiolated CDs than for unmodified CD. In vitro residence time on porcine intestine was prolonged 7-, 8.4-, and 7.9-fold for CD-SH, CD-SS-PEG 1 kDa, and CD-SS-PEG 2 kDa, respectively. In vivo results indicated CD-SS-PEG 1 kDa had the highest potential. Our comprehensive in vitro, ex vivo, and in vivo ffindings demonstrate that CD-SS-PEG 1 kDa is a highly promising candidate for mucoadhesive drug delivery systems.

Graphical Abstract