Novel amphiphilic probes for [18F]-radiolabeling preformed liposomes and determination of liposomal trafficking by positron emission tomography.
Positron-emission tomography (PET) is a noninvasive real-time functional imaging system and is expected to be useful for the development of new drug candidates in clinical trials. For its application with preformulated liposomes, we devised an optimized [18F]-compound and developed a direct liposome modification method that we termed the "solid-phase transition method". We were successful in using 1-[18F]fluoro-3,6-dioxatetracosane ([18F]7a) for in vivo trafficking of liposomes. This method might be a useful tool in preclinical and clinical studies of lipidic particle-related drugs.
Urakami
Takeo
T
Department of Medical Biochemistry and Global COE, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Akai
Shuji
S
Katayama
Yurie
Y
Harada
Norihiro
N
Tsukada
Hideo
H
Oku
Naoto
N
D000818:Animals; D005462:Fluorine Radioisotopes; D007553:Isotope Labeling; D008081:Liposomes / Q000737:chemistry* / Q000493:pharmacokinetics; D051379:Mice; D008807:Mice, Inbred BALB C; D010316:Particle Size; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics; D013501:Surface-Active Agents / Q000737:chemistry* / Q000506:poisoning; D014018:Tissue Distribution; D051598:Whole Body Imaging
D005462:Fluorine Radioisotopes; D008081:Liposomes; D019275:Radiopharmaceuticals; D013501:Surface-Active Agents