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Boron neutron capture therapy (BNCT) is a novel and emerging form of radiotherapy that combines the advantages of "heavy ion radiotherapy" and "biological targeting". The therapeutic potential of BNCT is ultimately constrained by precise and efficient delivery of boron drugs. In this review, we systematically trace from conventional boron drugs to sophisticated nano-delivery platforms, emphasizing breakthroughs in carrier engineering, targeted delivery strategies, and multifunctional synergistic systems. A dedicated analysis of the biological foundations, such as cell cycle dynamics, tumor microenvironmental interactions, and immunostimulatory effects, provides a crucial framework for understanding mechanism-informed biomaterial design. By synthesizing current advances with an outlook on future challenges, this work aims to chart a course for translating innovative boron-loaded biomaterials from the laboratory into clinical reality, thereby unlocking the full promise of BNCT.