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<p>Gemcitabine remains a vital chemotherapeutic agent, yet its rapid deamination and short systemic persistence necessitate improved delivery strategies. This study examines the interaction of GB with α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), and poly-β-cyclodextrin (poly-β-CD) using UV–Vis spectroscopy, fluorescence titrations, and multidimensional NMR. While α-CD shows only weak surface-level association, β-CD, HP-β-CD, and poly-β-CD form clear inclusion complexes, indicated by hyperchromic shifts, fluorescence enhancement, and ROESY cross peaks confirming the proximity of gemcitabine’s aromatic and sugar protons to the CD cavity. Among these systems, β-CD exhibits the strongest affinity, with a binding constant on the order of 10<sup>5</sup>&#xa0;L·mol<sup>−1</sup>, reflecting its optimal cavity fit for GB. The biological relevance of these interactions was assessed using MCF-7 breast cancer cells. Although free gemcitabine shows the highest potency, the CD-based formulations retain significant activity while offering a moderated release profile. Notably, the poly-β-CD complex demonstrates improved cytotoxic performance among the CD carriers, with its IC<sub>50</sub> positioned near 11&#xa0;μg·mL<sup>−1</sup>, suggesting more efficient drug presentation compared to other complexes. Together, these findings highlight how subtle differences in cyclodextrin structure influence gemcitabine encapsulation, stability, and cellular response, positioning poly-β-CD as a promising platform for improved GB delivery.</p>

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Poly-β-Cyclodextrin as a Superior Host for Gemcitabine: Comparative Supramolecular Characterization and Anticancer Evaluation

  • 期刊论文

  • 发表日期：

    2026年5月30日

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  • Manickam Sathya,
  • Archana Sumohan Pillai,
  • Varnitha Manikantan,
  • Sengodan Amudha,
  • Ujma Ashapak Tamboli,
  • Ramaraj Rajesh Kumar,
  • Aleyamma Alexander,
  • Israel V. M. V. Enoch

摘要

Gemcitabine remains a vital chemotherapeutic agent, yet its rapid deamination and short systemic persistence necessitate improved delivery strategies. This study examines the interaction of GB with α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), and poly-β-cyclodextrin (poly-β-CD) using UV–Vis spectroscopy, fluorescence titrations, and multidimensional NMR. While α-CD shows only weak surface-level association, β-CD, HP-β-CD, and poly-β-CD form clear inclusion complexes, indicated by hyperchromic shifts, fluorescence enhancement, and ROESY cross peaks confirming the proximity of gemcitabine’s aromatic and sugar protons to the CD cavity. Among these systems, β-CD exhibits the strongest affinity, with a binding constant on the order of 105 L·mol−1, reflecting its optimal cavity fit for GB. The biological relevance of these interactions was assessed using MCF-7 breast cancer cells. Although free gemcitabine shows the highest potency, the CD-based formulations retain significant activity while offering a moderated release profile. Notably, the poly-β-CD complex demonstrates improved cytotoxic performance among the CD carriers, with its IC50 positioned near 11 μg·mL−1, suggesting more efficient drug presentation compared to other complexes. Together, these findings highlight how subtle differences in cyclodextrin structure influence gemcitabine encapsulation, stability, and cellular response, positioning poly-β-CD as a promising platform for improved GB delivery.