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[Display omitted] Boron neutron capture therapy (BNCT), as an innovative radiotherapy technology, has demonstrated remarkable outcomes when compared to conventional treatments in the management of recurrent and refractory brain tumors. However, in BNCT of brain tumors, the blood–brain barrier is a main stumbling block for restricting the transport of boron drugs to brain tumors, while the tumor targeting and retention of boron drugs also affect the BNCT effect. This review focuses on the recent development of strategies for delivering boron drugs crossing the blood–brain barrier and targeting brain tumors, providing new insights for the development of efficient boron drugs for the treatment of brain tumors. [ABSTRACT FROM AUTHOR]