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Pak J Pharm Sci ; 31(4(Supplementary)): 1495-1499, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30058541

RESUMO

Bacterial infection is one of the vital sources of morbidity and mortality. The development of single photon emission computed tomography (SPECT) radiotracer agents using antibiotics, for targeting in-vivo bacteria, helps in antibiotic dose calibration, targeted infection therapy and reduction in mortality rate. The aim of this study was to appraised 99mTc-labeling sulfadiazine as a radiopharmaceutical for bacillus infections imaging. Radiolabeling of sulfadiazine with technetium-99m was carried out by subsequent addition of 1.5 mL aqueous solution of sulfadiazine (1mg/mL), 120µg stannous tartrate, gentistic acid as stabilizing agent and 185 MBq normal saline solution of 99mTcO4-1 (pertechnetate) at pH = 5. The reaction mixture was incubated for 40 min at room temperature with light stirring. The quality control analysis (ITLC-SG and paper chromatography analysis) revealed ~ 98% labeling yield. Biodistribution and scintigraphic study was carried using bacillus bacterial infection induced New Zealand white rabbits. Due to the ease of 99mTc-sulfadiazine conjugation method, high labeling efficiency, shelf stability (>95% up to 6h), blood serum stability (~90% up to 6h) and high uptake in the infected muscle (T/NT =2.21 at 1H), 99mTc-SDZ could be used as radiopharmaceutical of choice for further pre-clinical and clinical studies.


Assuntos
Antibacterianos/metabolismo , Bacillus , Modelos Animais de Doenças , Infecções por Bactérias Gram-Positivas/metabolismo , Sulfadiazina/metabolismo , Tecnécio/metabolismo , Animais , Antibacterianos/uso terapêutico , Bacillus/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos/métodos , Infecções por Bactérias Gram-Positivas/diagnóstico por imagem , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Humanos , Masculino , Tomografia por Emissão de Pósitrons/métodos , Coelhos , Sulfadiazina/uso terapêutico , Tecnécio/administração & dosagem , Distribuição Tecidual/efeitos dos fármacos , Distribuição Tecidual/fisiologia , Tomografia Computadorizada de Emissão de Fóton Único/métodos
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