Synthesis and biological evaluation of technetium-sarafloxacin complex for infection imaging

M. E. Moustapha; M. A. Motaleb; H. Shweeta; Mahmoud Farouk

doi:10.1007/s10967-015-4188-0

Synthesis and biological evaluation of technetium-sarafloxacin complex for infection imaging

M. E. Moustapha
, M. A. Motaleb
, H. Shweeta
, Mahmoud Farouk

Chemistry

Research output: Contribution to journal › Article › peer-review

8 Scopus citations

Abstract

Technetium-99m-sarafloxacin was synthesized and formulated for the development of a potential diagnostic imaging agent for the bacterial infection and inflammation with higher efficiency than the commercially available ^99mTc-ciprofloxacin. Factors influencing the labeling yield such as sarafloxacin amount, pH of the labeling reaction, SnCl₂ amount and reaction time were optimized. The labeled drug was subjected to preclinical evaluations in mice. The biodistribution studies indicated that ^99mTc-sarafloxacin displayed relatively high uptake in the infectious lesion (T/NT = 4.2 ± 0.1) at 2 h post-injection. The results revealed that ^99mTc-sarafloxacin cannot discriminate infection from sterile inflammation.

Original language	English
Pages (from-to)	699-705
Number of pages	7
Journal	Journal of Radioanalytical and Nuclear Chemistry
Volume	307
Issue number	1
DOIs	https://doi.org/10.1007/s10967-015-4188-0
State	Published - 1 Jan 2016

Keywords

Diagnosis
Infection
Inflammation
Labeling
Sarafloxacin

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10.1007/s10967-015-4188-0

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title = "Synthesis and biological evaluation of technetium-sarafloxacin complex for infection imaging",

abstract = "Technetium-99m-sarafloxacin was synthesized and formulated for the development of a potential diagnostic imaging agent for the bacterial infection and inflammation with higher efficiency than the commercially available 99mTc-ciprofloxacin. Factors influencing the labeling yield such as sarafloxacin amount, pH of the labeling reaction, SnCl2 amount and reaction time were optimized. The labeled drug was subjected to preclinical evaluations in mice. The biodistribution studies indicated that 99mTc-sarafloxacin displayed relatively high uptake in the infectious lesion (T/NT = 4.2 ± 0.1) at 2 h post-injection. The results revealed that 99mTc-sarafloxacin cannot discriminate infection from sterile inflammation.",

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AU - Moustapha, M. E.

AU - Motaleb, M. A.

AU - Shweeta, H.

AU - Farouk, Mahmoud

PY - 2016/1/1

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N2 - Technetium-99m-sarafloxacin was synthesized and formulated for the development of a potential diagnostic imaging agent for the bacterial infection and inflammation with higher efficiency than the commercially available 99mTc-ciprofloxacin. Factors influencing the labeling yield such as sarafloxacin amount, pH of the labeling reaction, SnCl2 amount and reaction time were optimized. The labeled drug was subjected to preclinical evaluations in mice. The biodistribution studies indicated that 99mTc-sarafloxacin displayed relatively high uptake in the infectious lesion (T/NT = 4.2 ± 0.1) at 2 h post-injection. The results revealed that 99mTc-sarafloxacin cannot discriminate infection from sterile inflammation.

AB - Technetium-99m-sarafloxacin was synthesized and formulated for the development of a potential diagnostic imaging agent for the bacterial infection and inflammation with higher efficiency than the commercially available 99mTc-ciprofloxacin. Factors influencing the labeling yield such as sarafloxacin amount, pH of the labeling reaction, SnCl2 amount and reaction time were optimized. The labeled drug was subjected to preclinical evaluations in mice. The biodistribution studies indicated that 99mTc-sarafloxacin displayed relatively high uptake in the infectious lesion (T/NT = 4.2 ± 0.1) at 2 h post-injection. The results revealed that 99mTc-sarafloxacin cannot discriminate infection from sterile inflammation.

KW - Diagnosis

KW - Infection

KW - Inflammation

KW - Labeling

KW - Sarafloxacin

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Synthesis and biological evaluation of technetium-sarafloxacin complex for infection imaging

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Keywords

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