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Purpose <p>This study aimed to enhance the therapeutic efficacy of the anticancer drug WEG-104, a selective inhibitor of carbonic anhydrase (CA) isoforms IX and XII, by developing and evaluating its delivery via poly(lactic-co-glycolic acid)-coated gold nanoparticles (GNPs) with two distinct morphologies: spheres and rods, inspired by the impact of morphology on cellular uptake and residence time within cells.</p> Methods <p>Spherical and rod-shaped GNPs were loaded with WEG-104 and characterized for size, surface charge, and encapsulation efficiency using techniques like Fourier transform-infrared spectroscopy. The antitumor activity of the nanoformulations was evaluated in vivo using an Ehrlich ascites carcinoma model, assessing tumor weight/volume, histology, concentrations of key proteins (HIF-1α, MMP-9, VEGF, caspase-9) and the expression of CA IX and XII genes compared to the free drug.</p> Results <p>Both nanoformulations demonstrated exceptionally high drug encapsulation (&gt; 95%). In vivo, WEG-104-loaded GNPs significantly outperformed the free drug, reducing tumor growth and viability while modulating cancer-related protein expression. Notably, spherical GNPs showed superior antitumor activity compared to nanorods, likely due to better tumor accumulation via the enhanced permeation and retention effect.</p> Conclusion <p>Incorporating WEG-104 into GNPs, particularly spherical ones, significantly improves its antitumor efficacy. This work highlights that tailoring nanoparticle morphology is a promising strategy for enhancing the therapeutic outcomes of drug delivery systems.</p>

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Boosting the Anticancer Effect of a Carbonic Anhydrase Inhibitor Through Loading Onto Gold Nanoparticles: In Vitro and In Vivo Assessment

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月6日

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  • Wagdy M. Eldehna,
  • Mahmoud A. El Hassab,
  • Rana A. Eissa,
  • Esraa B. Abdelazim,
  • Nahla A. Abdelshafi,
  • Mamdouh A. Oraby,
  • Ahmed S. Doghish,
  • Mohamed A. Elkady,
  • Rofaida Salem,
  • Elbadawy A. Kamoun,
  • Mahmoud Elsabahy,
  • Noura G. Eissa

摘要

Purpose

This study aimed to enhance the therapeutic efficacy of the anticancer drug WEG-104, a selective inhibitor of carbonic anhydrase (CA) isoforms IX and XII, by developing and evaluating its delivery via poly(lactic-co-glycolic acid)-coated gold nanoparticles (GNPs) with two distinct morphologies: spheres and rods, inspired by the impact of morphology on cellular uptake and residence time within cells.

Methods

Spherical and rod-shaped GNPs were loaded with WEG-104 and characterized for size, surface charge, and encapsulation efficiency using techniques like Fourier transform-infrared spectroscopy. The antitumor activity of the nanoformulations was evaluated in vivo using an Ehrlich ascites carcinoma model, assessing tumor weight/volume, histology, concentrations of key proteins (HIF-1α, MMP-9, VEGF, caspase-9) and the expression of CA IX and XII genes compared to the free drug.

Results

Both nanoformulations demonstrated exceptionally high drug encapsulation (> 95%). In vivo, WEG-104-loaded GNPs significantly outperformed the free drug, reducing tumor growth and viability while modulating cancer-related protein expression. Notably, spherical GNPs showed superior antitumor activity compared to nanorods, likely due to better tumor accumulation via the enhanced permeation and retention effect.

Conclusion

Incorporating WEG-104 into GNPs, particularly spherical ones, significantly improves its antitumor efficacy. This work highlights that tailoring nanoparticle morphology is a promising strategy for enhancing the therapeutic outcomes of drug delivery systems.