Radiosynthesis and characterization of the 99mTc-fleroxacin complex: a novel Escherichia coli infection imaging agent

Abstract

Radiocomplexation of fleroxacin (FXN) with technetium-99m and its characterization in terms of in vitro stability in saline and serum solutions, in vitro binding with live and heat-killed Escherichia coli, and biodistribution in male Wistar rats (MWR) artificially infected with live and heat-killed E. coli was studied. The 99m Tc-FXN complex showed a radiochemical purity (RCP) yield of 98.10 ± 0.24% at 30 min using 125 lg of stannous fluoride, 74 MBq of sodium pertechnetate, and 2 mg of FXN. The complex was found to be more than 90% stable up to 4 h after constitution in normal saline. In serum, the emergence of 16.50% undesirable species was observed within 16 h of incubation at 37°C. The 99m Tc-FXN complex showed saturated in vitro binding with E. coli with a maximum value of 65.00% at 90 min. A fivefold increase in uptake of the complex was noted in the infected when compared with the inflamed and normal muscle of the MWR infected with live E. coli. The stable radiochemical profile in saline and serum, saturated in vitro binding with E. coli and increased uptake in the infected muscle, confirmed the potential of the 99m Tc-FXN complex as an E. coli infection imaging agent.

Quantitative structure–activity relationship analysis to elucidate the clearance mechanisms of Tc-99m labeled quinolone antibiotics

“…Experimental data of the liver and kidney uptakes of 21 Tc99m labeled quinolone antibiotics were taken from the recently published papers [14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30]. The biodistribution data collected was reported in rats and mice and experimentally induced infection using Staphylococcus aureus or E. coli, after two hours of bacterial induction.…”

99mTc-Trimethoprim’in Radyosentezi ve Biyodağılımı: Deney Hayvanları Kullanılarak Bakteriyel Enfeksiyon Görüntüleme Için Yeni Bir Radyoişaretli Antibiyotik

“…Recently, some novel specific infection radiotracers have been developed, including ours, for localization and discrimination of infection from inflammation. The effectiveness of these radiopharmaceuticals has encouraged the development of novel and more specific agents [19][20][21][22][23][24][25][26] .…”

Radiosynthesis of 99mTc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer

“…Recently, some novel specific infection radiotracers have been developed, including ours, for localization and discrimination of infection from inflammation. The effectiveness of these radiopharmaceuticals has encouraged the development of novel and more specific agents [3][4][5][6][7][8][9][10][11].…”