Figure 4.
Pharmacokinetic profile, micro-PET imaging and biodistribution analysis in vivo. (A) Identification of F56-CM conjugated to albumin, before and after intravenous injection of 5 mg/kg F56-CM in BALB/c mice. Blood samples were taken at the indicated time points, diluted 1:50, and subjected to Western blot using the F56-specific antibody and the albumin-specific antibody. (B) The structures of radiolabeled 64Cu-DOTA-F56 and 64Cu-DOTA-F56-CM. (C-D) Micro-PET imaging of nu/nu mice bearing BCG-823 (C) and HT-29 (D) tumor cells. Images were acquired at 4 h after injection of 64Cu-DOTA-F56 and 64Cu-DOTA-F56-CM. Dotted circles indicate positions of tumors. (E-F) Biodistribution at 8 h after i.v. injection of 64Cu-DOTA-F56 and 64Cu-DOTA-F56-CM in nude mice xenografted with BGC-823 and HT-29 cells. Data were obtained using the radioactivity count method, plotted as % injected activity per gram of tissue (%IA/g). (G) Female Sprague-Dawley rats were given a single intravenous injection of 64Cu-DOTA-F56 or 64Cu-DOTA-F56-CM. Blood samples (20 µL) were collected before injection and up to 96 h after dosing and determined by gamma counting. Data represent mean ± SD of three independent experiments. *P < 0.05.