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Synthesis, biological evaluation and biodistribution of the 99m Tc–Garenoxacin complex in artificially infected rats

Synthesis, biological evaluation and biodistribution of the 99m Tc–Garenoxacin complex in... The labeling of garenoxacin (GXN) with technetium-99m ( 99m Tc) using different concentrations of GXN, sodium pertechnetate (Na 99m TcO 4 ), stannous chloride dihydrate (SnCl 2 ·2H 2 O) at different pH was investigated and evaluated in terms of in-vitro stability in saline, serum, binding with multi-resistant Staphylococcus aureus (MDRSA) and penicillin-resistant Streptococci (PRSC) and its biodistribution in artificially MDRSA and PRSC infected rats. 99m Tc–GXN complex with 97.45 ± 0.18% radiochemical stability was prepared by mixing 3 mg of GXN with 3 mCi of Na 99m TcO 4 in the presence of 150 μL of SnCl 2 ·2H 2 O (1 μg/μL in 0.01 N HCl) at a pH 5.6. The radiochemical stability of the complex was evaluated in normal saline up to 240 min of reconstitution. It was observed that the complex showed maximum RCP values after 30 min of the reconstitution and remained more than 90% up to 240 min. The complex showed radiochemical stability in normal saline at 37 °C up to 16 h with a 17.80% de-tagging. The complex showed saturated in-vitro binding with living MDRSA and PRSC as compared to the insignificant binding with heat killed MDRSA and PRSC. Biodistribution behavior of the complex was assessed in artificially infected with living and heat killed MDRSA and PRSC rats. It was observed that the accumulation of the complex in the infected (live MDRSA and PRSC) tissue of the rats was almost five fold than in the inflamed and normal tissue. The high radiochemical stability in normal saline at room temperature, promising in-vitro stability in serum at 37 °C, saturated in-vitro binding with living MDRSA and PRSC, specific biodistribution behavior and high infected (target) to normal (non-target) tissue and low inflamed (non-target) to normal (non-target) tissue ratios we recommend 99m Tc–GXN complex for in-vivo localization of infection caused by MDRSA and PRSC effective stains. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Radioanalytical and Nuclear Chemistry Springer Journals

Synthesis, biological evaluation and biodistribution of the 99m Tc–Garenoxacin complex in artificially infected rats

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References (27)

Publisher
Springer Journals
Copyright
Copyright © 2011 by Akadémiai Kiadó, Budapest, Hungary
Subject
Chemistry; Physical Chemistry ; Inorganic Chemistry ; Nuclear Physics, Heavy Ions, Hadrons; Nuclear Chemistry; Diagnostic Radiology
ISSN
0236-5731
eISSN
1588-2780
DOI
10.1007/s10967-010-0896-7
Publisher site
See Article on Publisher Site

Abstract

The labeling of garenoxacin (GXN) with technetium-99m ( 99m Tc) using different concentrations of GXN, sodium pertechnetate (Na 99m TcO 4 ), stannous chloride dihydrate (SnCl 2 ·2H 2 O) at different pH was investigated and evaluated in terms of in-vitro stability in saline, serum, binding with multi-resistant Staphylococcus aureus (MDRSA) and penicillin-resistant Streptococci (PRSC) and its biodistribution in artificially MDRSA and PRSC infected rats. 99m Tc–GXN complex with 97.45 ± 0.18% radiochemical stability was prepared by mixing 3 mg of GXN with 3 mCi of Na 99m TcO 4 in the presence of 150 μL of SnCl 2 ·2H 2 O (1 μg/μL in 0.01 N HCl) at a pH 5.6. The radiochemical stability of the complex was evaluated in normal saline up to 240 min of reconstitution. It was observed that the complex showed maximum RCP values after 30 min of the reconstitution and remained more than 90% up to 240 min. The complex showed radiochemical stability in normal saline at 37 °C up to 16 h with a 17.80% de-tagging. The complex showed saturated in-vitro binding with living MDRSA and PRSC as compared to the insignificant binding with heat killed MDRSA and PRSC. Biodistribution behavior of the complex was assessed in artificially infected with living and heat killed MDRSA and PRSC rats. It was observed that the accumulation of the complex in the infected (live MDRSA and PRSC) tissue of the rats was almost five fold than in the inflamed and normal tissue. The high radiochemical stability in normal saline at room temperature, promising in-vitro stability in serum at 37 °C, saturated in-vitro binding with living MDRSA and PRSC, specific biodistribution behavior and high infected (target) to normal (non-target) tissue and low inflamed (non-target) to normal (non-target) tissue ratios we recommend 99m Tc–GXN complex for in-vivo localization of infection caused by MDRSA and PRSC effective stains.

Journal

Journal of Radioanalytical and Nuclear Chemistry – Springer Journals

Published: Apr 1, 2011

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