Polyethylene glycol complexed with boronophenylalanine as a potential alternative to fructose-boronophenylalanine complexation to increase cellular uptake for BNCT Treatment

Boron Neutron Capture Therapy (BNCT) is a novel precision radiotherapy. The key to BNCT application lies in the effective targeting and retention of the boron-10 ( polyethylene glycol 400 and BPA were added to methanol and stirred until completely dissolved. The solution was then evaporated to remove methanol, yielding a pale-yellow clear liquid of PEG400-BPA complex. This complex was then used for in vitro and in vivo experiments, and it was evaluated for inhibition effects after BNCT irradiation in GL261 cells. Compared to the clinically used fructose-BPA, PEG400-BPA increased the boron uptake in tumor cells nearly twice and exhibit a better tumor-to-normal tissue ratio (T/N) in the We discovered that PEG400 can form a complex with BPA, significantly improving its water solubility. It provides a simple, long-term stable, easily convertible, and injectable formulation method for the delivery of BPA in BNCT treatment. It also offers new insights for BPA solubilization and formulation as well as compound forms of administration of boron drugs on the delivery of boron drugs in BNCT.