【摘要】 硼中子捕获疗法(boron neutron capture therapy, BNCT)作为一种前景广阔的恶性肿瘤治疗方法已经进入临床。硼药的肿瘤靶向是实现BNCT的二元细胞级精准靶向治疗的前提。基于肿瘤细胞表面特异性/差异性表达受体介导的选择性识别、靶向和富集是目前硼药靶向递送研究的焦点，同时还衍生出了一些精准靶向细胞器的其他靶向递送策略。本文在此分别从小分子硼药和纳米硼药的研发过程，解析了BNCT硼药靶向和递送方法的选择、挑战及其改进方案。新技术、新方法和新思路为未来分子靶向硼药、多靶向硼药的发展提供巨大的便利，包括：依赖组学技术的靶点寻找，依赖机器学习的靶向分子设计和优化，以及基于这些靶点库和靶向分子库搭建的模块化硼核的建立。更多还原

【Abstract】 Boron neutron capture therapy(BNCT) is a promising therapeutic method for malignant tumors and has entered the clinical trials. As a binary cellular accurate therapy, BNCT relies on tumor-targeting boron delivery. It is intriguing for boron delivery design that selective recognization, target, and accumulation are based on specific or differential expression receptors on the tumor cell surface. Several delivery strategies targeting other subcellular organelles have also emerged. Here, we summarized the selection, challenges, and improvement of boron targeting delivery methods in small molecule boron drugs and boron-containing nanoparticles. In the future, new technologies, new methods, and new ideas include target receptors finding via omics, ligands optimization via machine learning, and establishment of modular boron cores based on receptors and ligands libraries, thereby provide great convenience for the development of molecular-targeted boron drugs and multi-targeted boron drugs.更多还原