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<p>Chrysin (CHR), a naturally occurring flavonoid with promising anticancer potential, suffers from poor water solubility, limiting its therapeutic applications. To address this, β-Cyclodextrin (β-CD) inclusion complexes (ICs) of CHR were synthesized via the freeze-drying method at varying molar ratios (1:1, 1:2, 1:3, 1:4), with the 1:4 ratio exhibiting the highest entrapment efficiency (95.23%) and selected for further study. These ICs were then functionalized onto gold nanoparticles (AuNPs) to develop CHR-β-CD-AuNPs, enhancing drug delivery and stability. Characterization by UV–Vis, FTIR, NMR, NTA, and TEM confirmed successful encapsulation, hydrogen bonding, and spherical morphology with an average particle size of ~ 43&#xa0;nm. Molecular docking supported strong interactions between CHR and β-CD. In vitro studies against human triple-negative breast cancer (MDA-MB-231) cells demonstrated that CHR-β-CD-AuNPs exhibited potent cytotoxicity with an IC<sub>50</sub> of 22.17 ± 1.24&#xa0;mg/L, significantly lower than CHR/β-CD ICs (IC<sub>50</sub>: 22.84 ± 1.00&#xa0;mg/L) and free CHR (IC<sub>50</sub> &gt; 100&#xa0;mg/L, <i>p</i> &lt; 0.001). Hoechst and phalloidin staining revealed clear apoptotic features such as nuclear fragmentation and cytoskeletal disruption. Gene expression analysis showed upregulation of Bax and Caspase-3 and downregulation of Bcl-2, confirming apoptosis induction. Furthermore, scratch wound assays demonstrated significant inhibition of cancer cell migration, with wound closure reduced to 8.38 ± 0.74% (IC) and 15.27 ± 1.05% (IC-AuNPs) compared to 74.41 ± 1.22% in untreated controls (<i>p</i> &lt; 0.001). These findings establish that β-CD-based CHR-AuNP nanocarriers substantially improve the solubility, stability, and therapeutic efficacy of CHR, offering a promising nanoformulations strategy for enhanced targeted breast cancer therapy.</p>

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Gold nanoparticles capped with inclusion complex for the delivery of Chrysin in triple-negative breast cancer

  • 期刊论文

  • 发表日期：

    2025年8月23日

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  • Kamini Velhal,
  • Parvindar Sah,
  • Rajesh Raut,
  • Smitali Patil,
  • Sagar Barage,
  • Jaya Lakkakula,
  • Imran Uddin

摘要

Chrysin (CHR), a naturally occurring flavonoid with promising anticancer potential, suffers from poor water solubility, limiting its therapeutic applications. To address this, β-Cyclodextrin (β-CD) inclusion complexes (ICs) of CHR were synthesized via the freeze-drying method at varying molar ratios (1:1, 1:2, 1:3, 1:4), with the 1:4 ratio exhibiting the highest entrapment efficiency (95.23%) and selected for further study. These ICs were then functionalized onto gold nanoparticles (AuNPs) to develop CHR-β-CD-AuNPs, enhancing drug delivery and stability. Characterization by UV–Vis, FTIR, NMR, NTA, and TEM confirmed successful encapsulation, hydrogen bonding, and spherical morphology with an average particle size of ~ 43 nm. Molecular docking supported strong interactions between CHR and β-CD. In vitro studies against human triple-negative breast cancer (MDA-MB-231) cells demonstrated that CHR-β-CD-AuNPs exhibited potent cytotoxicity with an IC50 of 22.17 ± 1.24 mg/L, significantly lower than CHR/β-CD ICs (IC50: 22.84 ± 1.00 mg/L) and free CHR (IC50 > 100 mg/L, p < 0.001). Hoechst and phalloidin staining revealed clear apoptotic features such as nuclear fragmentation and cytoskeletal disruption. Gene expression analysis showed upregulation of Bax and Caspase-3 and downregulation of Bcl-2, confirming apoptosis induction. Furthermore, scratch wound assays demonstrated significant inhibition of cancer cell migration, with wound closure reduced to 8.38 ± 0.74% (IC) and 15.27 ± 1.05% (IC-AuNPs) compared to 74.41 ± 1.22% in untreated controls (p < 0.001). These findings establish that β-CD-based CHR-AuNP nanocarriers substantially improve the solubility, stability, and therapeutic efficacy of CHR, offering a promising nanoformulations strategy for enhanced targeted breast cancer therapy.