Radiolabeling, characterization, and preclinical evaluation of plazomicin: A potential tracer for bacterial infection

In this study, 99mTc–plazomicin, a new radio‐antibiotic complex, was prepared specifically for bacterial infection localization and monitoring. Factors affecting the labeling reaction were studied and optimized to obtain a high yield (98.8 ± 0.2%). In silico, radiochemical and physicochemical charac...

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Bibliographic Details
Published in:Chemical biology & drug design 2022-05, Vol.99 (5), p.688-702
Main Authors: El‐kawy, O. A., Abdelaziz, G., Abdel‐Razek, A. S.
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
bacterial infection
Bacterial Infections - drug therapy
detection and localization of septic inflammation
Humans
plazomicin
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacology
Sisomicin - analogs & derivatives
Technetium - chemistry
technetium‐99m
Tissue Distribution
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Summary:In this study, 99mTc–plazomicin, a new radio‐antibiotic complex, was prepared specifically for bacterial infection localization and monitoring. Factors affecting the labeling reaction were studied and optimized to obtain a high yield (98.8 ± 0.2%). In silico, radiochemical and physicochemical characterization and biodistribution were performed to assess the complex aptness as a radiopharmaceutical. The complex was biologically evaluated in vitro using bacteria and in vivo using different inflammation models (sterile, bacterial, and fungal). Uptake in the bacterial model was highest (7.8 ± 0.3%). Results indicated that the technetium label did not alter the antibiotic biological behavior and backed the usefulness of 99mTc‐plazomicin as a potential tracer. 99mTc‐ plazomicin was developed, and its preliminary preclinical qualifications were assessed. At optimum conditions, the radiochemical yield was >98% and was stable over 20 h. the In silico, radiochemical and physicochemical characterization, in vitro assessment, and in vivo biodistribution using different inflammation models supported the usefulness of 99mTc‐plazomicin as a potential infection tracer.
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.14007