The One-Step Incorporation of Boron-10 Atom into Prostate Cancer-Targeted Fluorophores for Visualizing In Vivo Boron-10 Delivery and Intratumoral Distribution with Cellular Resolution.

To enable real-time imaging of boron delivery with cellular resolution, a series of fluorescent [10B] compounds was developed via a one-step synthesis using cost-effective, scalable reagents. The tumor-targeting agent, [10B]-a11, allowed noninvasive monitoring to identify the optimal time point for boron neutron capture therapy (BNCT) based on peak tumor accumulation. Fluorescence imaging analysis revealed a heterogeneous intratumoral distribution of [10B]-a11, confirming that macroscopic accumulation does not equate to microscopic uniformity and emphasizing the need for improved tumor penetration in next-generation boron carriers. Furthermore, [10B]-a11 demonstrated efficacy for fluorescence-guided surgery in prostate cancer, suggesting a potential synergistic strategy to combine precise resection with BNCT for improved therapeutic outcomes.