Journal
BIOPHYSICAL CHEMISTRY
Volume 111, Issue 1, Pages 27-34Publisher
ELSEVIER
DOI: 10.1016/j.bpc.2004.03.010
Keywords
BPA; BNCT; liposomes; NMR of lipid structures; DOTAP/DOPE
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Cationic liposomes are widely used as carriers of biomolecules specifically targeted to the cell nucleus. p-Boronphenylalanine (BPA) is a powerful anti-tumor agent for Boron Neutron Capture Therapy (BNCT). In this paper, H-1 and C-13 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 1,2-diolcoyi-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. (C) 2004 Published by Elsevier B.V.
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