Boronphenylalanine insertion in cationic liposomes for Boron Neutron Capture Therapy

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• 作者：Martini ; Silvia ; Ristori ; Sandra ; Pucci ; Amaranta ; Bonechi ; Claudia ; Becciolini ; Aldo ; Martini ; Giacomo ; et. al.
• 关键词：BPA ; BNCT ; Liposomes ; NMR of lipid structures ; DOTAP/DOPE
• 刊名：Biophysical Chemistry
• 出版年：2004
• 出版时间：September 1, 2004
• 年：2004
• 卷：111
• 期：1
• 页码：27-34
• 全文大小：427 K

文摘

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, 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 1,2-dioleoyl-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.