Emerging agents for boron neutron capture therapy: Biomolecular carriers paving the way for precision radiotherapy

作者：Chang Chen, Maosong Yang, J.H. Wang, Ling Zhang, Shaobo Huang, Xiao Xu, Yang Liu · 发表于：Precision Radiation Oncology · 年份：2026 · DOI：10.1002/pro6.70079 · 研究领域：Boron Compounds in Chemistry、Boron and Carbon Nanomaterials Research、Organoboron and organosilicon chemistry

Boron neutron capture therapy (BNCT) is an emerging targeted radiotherapy technology that enables precise eradication of tumor cells. The development of efficient boron carriers is crucial for the advancement of BNCT technology. Notably, biomolecular carriers currently represent the only class of drug carriers that has achieved market approval (e.g., boronophenylalanine [BPA] in Japan), underscoring their pivotal role in clinical applications. Their outstanding biocompatibility, high payload capacity, and tumor-targeting capabilities align closely with the stringent requirements of BNCT drug delivery. For instance, amino acid-based carriers (such as BPA) utilize L-type amino acid transporter 1 (LAT1) for tumor-specific accumulation; nucleoside prodrugs are activated by thymidine kinase 1 (TK1) and incorporated into tumor DNA; carbohydrate-based carriers improve solubility and targeting through glucose transporters (GLUTs); peptide carriers facilitate cellular uptake via receptor-mediated endocytosis or cell-penetrating peptides; and liposomes leverage the enhanced permeability and retention (EPR) effect together with active-targeting modifications for enhanced tumor delivery. Nevertheless, delivering ultrahigh doses of boron remains a major challenge. Biomacromolecules, particularly albumin-based systems, have garnered increasing attention because of their excellent biosafety and high boron-loading potential, offering promising avenues for overcoming dose delivery barriers in...