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Constructing dual-modality theranostic agents by fusing π-systems and σ-aromatic boron clusters: enhanced phototherapy and boron neutron capture therapy
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DOI：10.1007/s11426-026-3473-8.png)
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Abstract
En 中文
The development of innovative theranostic platforms that enable advanced therapies is crucial for advancing cancer treatment. Herein, we propose a molecular design integrating a π-conjugated luminogen with a boron cluster to create a hybrid agent for the combined and enhanced application of photothermal therapy (PTT) and boron neutron capture therapy (BNCT). As a proof of concept, we covalently anchored a nido-carborane cluster to a cyanine dye, constructing IRbiotin-nCB. Studies reveal the nido-carborane acts as an efficient photo-induced electron transfer (PET) donor, quenching fluorescence and enhancing the photothermal conversion efficiency to 33.9%—a significant improvement over the 23.9% efficiency of the parent cyanine. Furthermore, when evaluated as a boron delivery agent in vivo, IRbiotin-nCB demonstrated exceptional performance. At a low dose of 15 mg/kg, it achieved high tumor boron accumulation of 32.66 ± 0.85 µg/g, with superior selectivity evidenced by a tumor-to-blood ratio of 14.71 and tumor-to-normal tissue ratios consistently greater than 3. These values surpass the requisite thresholds for effective BNCT. By integrating optical activity for PTT and neutron capture capacity for BNCT within a single molecule, this hybrid platform enables a powerful synergistic therapy leading to complete tumor ablation, presenting a promising strategy for future cancer theranostics.
Keywords:
carboranes
boron cluster
NIR emission
phototherapy
boron neutron capture therapy
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