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.