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Objective <p>Boron neutron capture therapy (BNCT) is limited by inadequate boron delivery to tumor cells and the inability to visualize boron agents for personalized treatment. This study introduces DOTA-BPA-Gd, a dual-function boron agent integrating BNCT efficacy with drug tracing.</p> Methods <p>DOTA-BPA-Gd was designed with four phenylboronic acid groups to target sialic acid residues on cancer cell surfaces. This strategy aims to enhance tumor boron accumulation while avoiding LAT1-mediated exocytosis and transporter saturation associated with BPA-F. With a molecular weight of ~ 1200&#xa0;Da, DOTA-BPA-Gd allows efficient spatial binding to sialic acid, improving targeting specificity. Cellular uptake, cytotoxicity, and boron distribution were evaluated, followed by <i>in vivo</i> BNCT experiments with MRI monitoring.</p> Results <p>DOTA-BPA-Gd effectively delivered boron to cancer cells without detectable toxicity. Under neutron irradiation, the DOTA-BPA-Gd + N group showed significant tumor inhibition, with tumor volumes reduced to about one-third of those in the BPA-F + N group. Furthermore, gadolinium enabled real-time MRI-based tracking of boron biodistribution, confirming the agent’s dual functionality.</p> Conclusions <p>DOTA-BPA-Gd offers a promising strategy for BNCT by combining targeted boron delivery with non-invasive imaging. This integrated approach improves treatment precision, enhances therapeutic efficacy, and may help overcome key clinical challenges in BNCT.</p> Graphical Abstract <p></p>

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Spatial Targeting of Sialic Acid Receptors for MRI/BNCT-Integrated Boron Drug-Based Antitumor Therapy

  • 期刊论文

  • 发表日期：

    2026年2月28日

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  • Xiaoyan Sun,
  • Yaxin Qin,
  • Zhiqing Ben,
  • Zhicheng Zhang,
  • Xiaoyan Bao,
  • Yufan Yang,
  • Yongjie Shui,
  • Haiyan Chen,
  • Dang Wu,
  • Qichun Wei,
  • Min Han

摘要

Objective

Boron neutron capture therapy (BNCT) is limited by inadequate boron delivery to tumor cells and the inability to visualize boron agents for personalized treatment. This study introduces DOTA-BPA-Gd, a dual-function boron agent integrating BNCT efficacy with drug tracing.

Methods

DOTA-BPA-Gd was designed with four phenylboronic acid groups to target sialic acid residues on cancer cell surfaces. This strategy aims to enhance tumor boron accumulation while avoiding LAT1-mediated exocytosis and transporter saturation associated with BPA-F. With a molecular weight of ~ 1200 Da, DOTA-BPA-Gd allows efficient spatial binding to sialic acid, improving targeting specificity. Cellular uptake, cytotoxicity, and boron distribution were evaluated, followed by in vivo BNCT experiments with MRI monitoring.

Results

DOTA-BPA-Gd effectively delivered boron to cancer cells without detectable toxicity. Under neutron irradiation, the DOTA-BPA-Gd + N group showed significant tumor inhibition, with tumor volumes reduced to about one-third of those in the BPA-F + N group. Furthermore, gadolinium enabled real-time MRI-based tracking of boron biodistribution, confirming the agent’s dual functionality.

Conclusions

DOTA-BPA-Gd offers a promising strategy for BNCT by combining targeted boron delivery with non-invasive imaging. This integrated approach improves treatment precision, enhances therapeutic efficacy, and may help overcome key clinical challenges in BNCT.

Graphical Abstract