Boronphenylalanine Insertion in Cationic Liposomes for Boron Neutron Capture Therapy

Cationic liposomes are widely used as carriers of biomolecules specifically targeted to the cell nucleus. p-Boronphenylalanine (BPA) is powerful anti-tumor agent for Boron Neutron Capture Therapy (BNCT). In this paper, 1H and 13C NMR was used to study the insertion of BPA in mixed liposomes, made up by the positively charged 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) and the zwitterionic 1,2dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). The boronated drug was distributed between the water phase and the liposomes. The location site of BPA into the lipid bilayer was investigated and the boron-substituted aromatic ring was found inserted in the hydrophobic region, whereas the amino acidic group was oriented towards the aqueous environment. Further information was given by proton spin-lattice relaxation rates.