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Labelling of ceftriaxone with 99m Tc and its bio‐evaluation as an infection imaging agent
Author(s) -
Sohaib Muhammad,
Khurshid Zain,
Roohi Samina
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3235
Subject(s) - ceftriaxone , biodistribution , chemistry , scintigraphy , staphylococcus aureus , escherichia coli , inflammation , imaging agent , labelling , in vitro , microbiology and biotechnology , in vivo , antibiotics , pharmacology , bacteria , immunology , medicine , biochemistry , biology , gene , genetics
Differentiation of bacterial and sterile inflammation will have a significant impact on the current clinical practice. Ceftriaxone (CTRX) was labelled with 99m Tc and assessed for its ability to depict infection on scintigraphy. Stoichiometry was performed to optimize labelling parameters. Stability and bacterial binding was verified and biodistribution pattern was seen in normal, infected/inflamed animal models. 99m Tc‐CTRX prepared at pH 7 with stannous chloride of 50 µg, ligand of 30 mg, and boiling for 10 min gave labelling yield of 96.2 ± 0.2% with good stability. In vitro binding was higher for Escherichia coli than Staphylococcus aureus . Biodistribution in normal rats showed high uptake in hepatobiliary system, gut and urinary system. In animal models induced with infection or inflammation, lesion to normal ratios at 4 h were 2.36 ± 0.21, 12.66 ± 1.44 and 1.40 ± 0.01 with S . aureus infection, E . coli infection and turpentine oil inflammation, respectively. Infection specificity especially for E . coli was also confirmed on scintigraphic findings. Ceftriaxone can be labelled with 99m Tc with high labelling yield at pH compatible with that of blood. Our preparation has shown stability in vitro and in human serum, and binds preferentially with bacteria. 99m Tc‐CTRX scintigraphy can be used to delineate sites of active infection and to differentiate infection and inflammation.