PET imaging of liposomes labeled with an [18F]-fluorocholesteryl ether probe prepared by automated radiosynthesis
作者： Andreas Tue Ingemann Jensen , Tina Binderup , Thomas L. Andresen , Andreas Kjær , Palle H. Rasmussen
DOI: 10.3109/08982104.2012.698418
关键词: Pet imaging 、 Radiochemistry 、 Automated radiosynthesis 、 Ether 、 Chemistry 、 Pharmacokinetics 、 Biochemistry 、 Mesylate 、 Ether lipid 、 Liposome 、 Positron emission tomography
摘要: A novel [18F]-labeled cholesteryl ether lipid probe was prepared by synthesis of the corresponding mesylate, which [18F]-fluorinated a [18F]KF, Kryptofix-222, K2CO3 procedure. Fluorination done for 10 minutes at 165°C and took place with conversion between 3 17%, depending on conditions. Radiolabelling subsequent in situ purification SEP-Paks were custom-built, fully automatic robot. Long-circulating liposomes hydration (magnetic stirring) film containing radiolabeled probe, followed automated extrusion through 100-nm filters. The injected into nude, tumor-bearing mice, positron emission tomography (PET) scans performed several times over 8 hours to investigate vivo biodistribution. Clear tumor accumulation, as well hepatic splenic uptake, observed, expected liposomal pharmacokinetics. accumulation postinjection accounted...
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