Development of a thermal neutron-sensitive liposome for a novel drug delivery system aiming for radio-chemo-concurrent cancer therapy

Akamatsu, Ken

An ionizing radiation-sensitive liposome has been developed aiming for irradiation site-specific controlled release of an anticancer agent from liposomes accumulated at tumor. As the first step of the study, X-ray-sensitive liposome has been constructed, consisting of an unsaturated phosphatidyl choline (PC), a saturated PC, and cholesterol. The radiation sensitivity was estimated by measuring release rate of a fluorophore, calcein, through the lipid bilayer. As a result, the following characteristics of X-ray-sensitive liposomes were discovered: (1) A PC with bis-allylic hydrogen is an essential component of unsaturated PC, (2) Dilinoleoyl PC (DLOPC) is the most favorable component of unsaturated PC, (3) A lower dose rate makes the liposome more X-ray-sensitive. In this presentation, we will discuss radiation chemical mechanism of the ionizing radiation-sensitive liposome, and their pharmaceutical applications for radiation therapy such as boron neutron capture therapy.