Human Serum Albumin‐Coated ¹⁰B Enriched Carbon Dots as Targeted “Pilot Light” for Boron Neutron Capture Therapy

Boron neutron capture therapy (BNCT) is a physiologically focused radiation therapy that relies on nuclear capture and fission processes. BNCT is regarded as one of the most promising treatments due to its excellent accuracy, short duration of therapy, and low side effects. The creation of novel boron medicines with high selectivity, ease of delivery, and high boron-effective load is a current research topic. Herein, boron-containing carbon dots (BCDs) and their human serum albumin (HSA) complexes (BCDs-HSA) are designed and synthesized as boron-containing drugs for BNCT. BCDs (¹⁰B: 7.1 wt%) and BCDs-HSA exhibited excitation-independent orange fluorescent emission which supported the use of fluorescence imaging for tracking ¹⁰B in vivo. The introduction of HSA enabled BCDs-HSA to exhibit good biocompatibility and increased tumor accumulation. The active and passive targeting abilities of BCDs-HSA are explored in detail. Subcutaneous RM-1 tumors and B16-F10 tumors both significantly decrease with BNCT, which consists of injecting BCDs-HSA and then irradiating the area with neutrons. In short, this study provides a novel strategy for the delivery of boron and may broaden the perspectives for the design of boron-containing carbon dots nanomedicine for BNCT.