Record Details

99mTc-Labeling of Ciprofloxacin and Nitrofuryl Thiosemicarbazone Using Fac-[99mTc(CO)3(H2O)3] Core: Evaluation of Their Efficacy as Infection Imaging Agents

EPrints@IICB

View Archive Info
 
 
Field Value
 
Title 99mTc-Labeling of Ciprofloxacin and Nitrofuryl Thiosemicarbazone Using Fac-[99mTc(CO)3(H2O)3] Core: Evaluation of Their Efficacy as Infection Imaging Agents
 
Creator Halder, Kamal Krishna
Nayak, Dipak Kumar
Baishya, Rinku
Sarkar, Bharat R
Sinha, S
Ganguly, Shantanu
Chatterjee Debnath, Mita
 
Subject Infectious Diseases and Immunology
 
Description The aim of this study was to radiolabel ciprofloxacin (Cip) and nitrofuryl thiosemicarbazone (NFT) with the fac-[99mTc(CO)3(H2O)3]+ core and to evaluate the ability of the radiopharmaceuticals as tracers in detecting sites of infection. Cip and NFT were radiolabeled with the
fac-[99mTc(CO)3(H2O)3]+ core and characterized by RHPLC. The stabilities of the preparations were evaluated in saline and rat serum. In vitro binding studies of the radiopharmaceuticals with S. aureus were performed. Biodistribution studies were conducted at different time points after injecting (i.v.) the radiopharmaceuticals in rats (intramuscularly infected with S. aureus) as well as in rats with sterile inflammation. To assess the infection targeting capacity of 99mTc-tricarbonyl ciprofloxacin and
nitrofuryl thiosemicarbazone, 99mTc(V)O-Cip and 99mTc(V)O-NFT were used as control. Scintigraphic imaging studies of tricarbonyl compounds and 99mTc(V)O-Cip were performed at 4 h after injection. The radiochemical purities of 99mTc(CO)3-Cip and 99mTc(CO)3-NFT were between 97–98% as determined by thin layer chromatography (TLRC) and RHPLC; no further purification is necessary before injection. The radiopharmaceuticals exhibited substantial stability when incubated in isotonic saline and serum up to 24 h. Biodistribution studies showed maximum uptake in the infected rat thigh muscle at 4 h post injection and washing out at slower rate from the infected site than the oxo
technetium chelate. The mean ratios of uptake in infected/non–infected thighs were 3.87 : 1, 3.41 : 1 and
3.17 : 1 for 99mTc(CO)3-Cip, 99mTc(CO)3-NFT and 99mTc(V)O-Cip respectively. During scintigraphic studies, infection sites appeared quite distinctly with 99mTc(CO)3-Cip and 99mTc(CO)3-NFT, comparable to the behaviour with 99mTc(V)O-Cip. These results encouraged us for further development
of infection imaging radiopharmaceuticals based on the 99mTc-tricarbonyl core.
 
Date 2011
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/1591/1/N_C_Ghosh_4.pdf
Halder, Kamal Krishna and Nayak, Dipak Kumar and Baishya, Rinku and Sarkar, Bharat R and Sinha, S and Ganguly, Shantanu and Chatterjee Debnath, Mita (2011) 99mTc-Labeling of Ciprofloxacin and Nitrofuryl Thiosemicarbazone Using Fac-[99mTc(CO)3(H2O)3] Core: Evaluation of Their Efficacy as Infection Imaging Agents. Metallomics, 3. pp. 1041-1048.
 
Relation http://dx.doi.org/10.1039/c1mt00068c
http://www.eprints.iicb.res.in/1591/