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<p>Colorectal cancer is 3rd most common cancer globally. Regorafenib (RE) is administered orally for the treatment of colorectal cancer; however, it has certain limitations, <i>viz.</i>, poor solubility, low bioavailability, and high clearance. The present study explores the development of RE-loaded gold nanoparticles (REGNPs) to improve colorectal cancer therapy. The REGNPs were prepared using the Turkevich method and optimized by Box–Behnken design. HAuCl4 (mM), TSC (% w/v), and pH were selected as independent variables, and particle size, entrapment efficiency, and zeta potential were chosen as dependent variables. The optimized REGNPs showed a small particle size (18.4&#xa0;nm), high monodispersity, high zeta potential (-28.2 mV), and appropriate entrapment of RE (77.9%). The morphology was examined by TEM, which revealed a spherical shape and a smooth surface. Fourier-transform infrared spectroscopy showed high compatibility of RE with excipients. Differential scanning calorimetry showed strong drug binding or encapsulation by GNPs. In-vitro release studies demonstrated a sustained release profile of RE from the REGNPs. Evaluation of cytotoxicity in the HCT116 cell line revealed that the optimized REGNPs exhibited greater in-vitro antitumor activity than the pure RE dispersion. The IC50 of RE from REGNPs12 (4.04 ± 0.32 µM) was significantly lower (<i>P</i> &lt; 0.05) than that of pure RE dispersion (6.09 ± 0.58 µM) against the HCT 116 cell line, indicating better cytotoxicity. These results suggest that GNPs may serve as an effective drug delivery system for colorectal cancer, and further in-vivo studies are warranted to evaluate their potential.</p>

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Development of Regorafenib Conjugated Gold Nanoparticles for the Treatment of Colorectal Cancer: Box–Behnken Optimized, Characterization, and In-vitro Biological Study Against HCT116 Cell Line

  • 期刊论文

  • 发表日期：

    2026年5月4日

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  • Dibyalochan Mohanty,
  • Thaduri Bindu,
  • Ameeduzzafar Zafar,
  • Omar Awad Alsaidan,
  • Mohd Yasir

摘要

Colorectal cancer is 3rd most common cancer globally. Regorafenib (RE) is administered orally for the treatment of colorectal cancer; however, it has certain limitations, viz., poor solubility, low bioavailability, and high clearance. The present study explores the development of RE-loaded gold nanoparticles (REGNPs) to improve colorectal cancer therapy. The REGNPs were prepared using the Turkevich method and optimized by Box–Behnken design. HAuCl4 (mM), TSC (% w/v), and pH were selected as independent variables, and particle size, entrapment efficiency, and zeta potential were chosen as dependent variables. The optimized REGNPs showed a small particle size (18.4 nm), high monodispersity, high zeta potential (-28.2 mV), and appropriate entrapment of RE (77.9%). The morphology was examined by TEM, which revealed a spherical shape and a smooth surface. Fourier-transform infrared spectroscopy showed high compatibility of RE with excipients. Differential scanning calorimetry showed strong drug binding or encapsulation by GNPs. In-vitro release studies demonstrated a sustained release profile of RE from the REGNPs. Evaluation of cytotoxicity in the HCT116 cell line revealed that the optimized REGNPs exhibited greater in-vitro antitumor activity than the pure RE dispersion. The IC50 of RE from REGNPs12 (4.04 ± 0.32 µM) was significantly lower (P < 0.05) than that of pure RE dispersion (6.09 ± 0.58 µM) against the HCT 116 cell line, indicating better cytotoxicity. These results suggest that GNPs may serve as an effective drug delivery system for colorectal cancer, and further in-vivo studies are warranted to evaluate their potential.