Design of Boron lipids and its Application to Boron Nano Capsules on Neutron Capture Therapy

摘要

Boron neutron capture therapy (BNCT) is a binary cancer treatment based on the nuclear reaction of two essentially nontoxic species, ~(10)B and thermal neutrons, and high accumulation and selective delivery of boron into tumor tissue are the most important requirements to achieve efficient BNCT. We have focused on boronated liposomes for boron delivery system. We recently developed the nido-carborane lipid, which has a double-tailed moiety conjugated with nido-carborane as a hydrophilic function. We investigated active targeting of the boronated liposomes to solid tumors by conjugation of transferrin onto the surface of their liposomes and achieved a boron concentration of 22 μg ~(10)B/g tumor by the injection of the liposomes at 7.2 mg ~(10)B/kg body weight with longer survival rates of tumor bearing mice after BNCT. However, the mice injected at higher boron concentrations resulted in mortality.