Radiosynthesis of 99mTc-nitrofurantoin a novel radiotracer for in vivo imaging of Escherichia coli infection

• Published in: Journal of radioanalytical and nuclear chemistry 2011-02, Vol.287 (2), p.417-422
• Main Authors: Shah, Syed Qaiser, Khan, Aakif Ullah, Khan, Muhammad Rafiullah
• Format: Article
• Language: English
• Subjects: Chemistry; Chemistry and Materials Science; Diagnostic Radiology; Escherichia coli; Hadrons; Heavy Ions; Inorganic Chemistry; Nuclear Chemistry; Nuclear Physics; Physical Chemistry
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-010-0697-z

Nitrofurantoin (NFN) radiolabeling with technetium-99m ( 99m Tc) was investigated using different concentration of the NFN, sodium pertechnetate (Na 99m TcO 4 ), reducing agent (SnCl 2 ) at different pH ranges (5.1–6.00). The suitability of the 99m Tc-NFN was evaluated in terms of the radiochemical purity (RCP) yield, in vitro stability in saline, serum, in vitro binding with E. coli , biodistribution in E. coli infected model rat (ERT), and scintigraphic accuracy in E. coli infected model rabbit (EBT). The superlative radiochemical succumb at 2.5 mg NFN, 125 μL of SnCl 2 (1 μg/μL in 0.01 N HCl), 2.5 mCi of Na 99m TcO 4 , at pH 5.2 at 30, 60, 90, and 120 min after reconstitution was 64.50 ± 0.11, 97.50 ± 0.16, 94.25 ± 0.10, 92.15 ± 0.14 and 90.75 ± 0.0.13%. The complex was found stable in saline and serum for 90% up to 120 min and showed 50–65% in vitro binding with E. coli . The absorption of the 99m Tc-NFN, primarily at E. Coli infected (ECT) muscle of ERT was lower but after 60 min it went up to 7.25 ± 0.17%. The absorption in the blood, liver, spleen, stomach, intestines, inflamed muscle (N.T1) and normal muscle (N.T2) went down while in the kidney and urine it went up with time. The ratio of the ECT/N.T1 was 7:1 and N.T2/N.T1 was 2:1. The Whole Body Static (WBS) imaging of the ERB confirmed the suitability of the 99m Tc-NFN as radiotracer. The superlative radiochemical succumb, significant in vitro stability in saline and serum, in vitro binding with E. coli , ideal biodistribution and scintigraphic accuracy confirmed the viability of the 99m Tc-NFN as radiotracer for infection.