LAUSR

&NA; Boron neutron capture therapy is a promising tumor treatment method, though its wide application has been limited due to the poor tumor selectivity and intracellular delivery of 10B‐compounds. Here, block copolymer‐boron cluster conjugate based on the clinically used sodium borocaptate (BSH) and poly(ethylene glycol)‐b‐poly(glutamic acid) copolymer have been developed for effectively penetrating tumor tissues and homogeneously delivering the boron clusters into cancer cells towards safe and efficient boron neutron capture therapy. The PEGylated block copolymer‐boron cluster (BSH) conjugate has demonstrated significant higher cellular uptake and tumor accumulation when compared to the non‐PEGylated formulations and BSH. Moreover, the enhanced delivery to tumors of the conjugates, as well as their superior intratumoral penetration, which facilitated reaching the intracellular space of most cells in tumors, allowed the effective ablation of tumors after neutron irradiation.