Preparation, nano purification, quality control and labeling optimization of [64Cu]-5,10,15,20-tetrakis (penta fluoro phenyl) porphyrin complex as a possible imaging agent

• Published in: Journal of radioanalytical and nuclear chemistry 2013-01, Vol.295 (1), p.255-263
• Main Authors: Fazaeli, Yousef, Jalilian, Amir R., Amini, Mostafa M., Aboudzadeh, Mohammadreza, Feizi, Shahzad, Rahiminezhad, Ali, Yousefi, Kamran
• Format: Article
• Language: English
• Subjects: Chemistry; Chemistry and Materials Science; Copper; Diagnostic Radiology; Hadrons; Heavy Ions; Imaging; Inorganic Chemistry; Nanocomposites; Nanomaterials; Nanostructure; Nuclear Chemistry; Nuclear Physics; Physical Chemistry; Porphyrins; Purification; Purity
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-012-1885-9

Cu-64 was produced via the 68 Zn (p,αn) 64 Cu nuclear reaction (≈200 mCi, >95 % chemical yield at 180 μA for 1.1 h irradiation, (radionuclidic purity >96 %, copper-67 as impurity) followed by purification with amino functionalized nano magnetic oxide, Fe 3 O 4 aiming to remove trace amount of heavy metal ions from aqueous media due to achieve ultra pure [ 64 Cu] CuCl 2 for labeling step. [ 64 Cu] labeled 5,10,15,20-tetrakis(penta fluoro phenyl) porphyrin ([ 64 Cu]-TFPP) was prepared using freshly prepared [ 64 Cu] CuCl 2 (Cu-64; T 1/2  = 12.7 h) and 5,10,15,20-tetrakis(penta fluoro phenyl)porphyrin (H 2 TFPP) for 60 min at 100 °C under reflux condition (radiochemical purity: >97 % ITLC, >98 % HPLC, specific activity: 14–16 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 24 h. The partition coefficient was calculated for the compound (log P  = 0.73). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and PET imaging up in 2 and 4 h after injection. A detailed comparative pharmacokinetic study performed for 64 Cu cation and [ 64 Cu]-TFPP. The complex is mostly washed out from the circulation through kidneys and liver and can be an interesting tumor imaging/targeting agent due to high specific uptake and rapid excretion through the urinary tract.