Department of Chemistry, Government College University, Faisalabad, Pakistan.
Isotope Production Division (IPD), Pakistan Institute of Nuclear Science and Technology (PINSTECH), Nilore, Islamabad, Pakistan.
Chem Biol Drug Des. 2019 Feb;93(2):154-162. doi: 10.1111/cbdd.13393. Epub 2018 Oct 31.
The development of functional imaging is a promising strategy for diagnosis and treatment of infectious and cancerous diseases. In this study, epirubicin was developed as a [ Tc]-labeled radiopharmaceutical for the imaging of multi-drug-resistant Staphylococcus aureus infections. The labeling was carried out using sodium pertechnetate (Na TcO ; ~370 MBq). The other parameters such as amount of ligand, reducing agent (SnCl .2H O), and pH were optimized. The highest labeling yield ≥96.98% was achieved when 0.3 mg epirubicin, 13 μg SnCl .2H O, and ~370 MBq Na TcO were incubated at pH 7 for 15 min in the presence of ascorbic acid at room temperature. Radiochemical purity, stability, charge, and glomerular filtration rate were studied to evaluate the biological compatibility for in vivo administration. Biodistribution investigations showed radiotracer uptake (13.89 ± 1.56% ID/gm organ) by liver and 7.79 ± 0.38% ID/gm organ by kidneys at 30 min post-injection which promisingly wash out at 24 hr post-injection. Scintigraphy study showed selective uptake in S. aureus-infected tissues in contrast to turpentine oil-induced inflamed tissues. Target-to-non-target ratio (6.7 ± 0.05) was calculated at 1 hr post-injection using SPECT gamma camera. The results of this study reveal that the [ Tc]-epirubicin can be a choice of imaging and monitoring the treatment process of multi-drug resistant S. aureus bacterial infections.
功能成像的发展是诊断和治疗传染性和癌症疾病的一种有前途的策略。在这项研究中，表阿霉素被开发为一种[Tc]标记放射性药物，用于多药耐药金黄色葡萄球菌感染的成像。标记是使用高锝酸钠（NaTcO4；370MBq）进行的。其他参数，如配体的量、还原剂（SnCl2·2H2O）和pH值都进行了优化。当 0.3mg 表阿霉素、13μg SnCl2·2H2O 和370MBq NaTcO4在室温下用抗坏血酸孵育 15 分钟时，获得了最高标记产率≥96.98%。放射性化学纯度、稳定性、荷电性和肾小球滤过率都进行了研究，以评估体内给药的生物相容性。生物分布研究表明，放射性示踪剂在 30 分钟时通过肝脏摄取（13.89±1.56%ID/gm 器官），通过肾脏摄取（7.79±0.38%ID/gm 器官），在 24 小时时很好地清除。闪烁照相研究表明，在感染金黄色葡萄球菌的组织中有选择性摄取，而在松节油诱导的炎症组织中则没有。使用 SPECT 伽马相机在 1 小时时计算了靶与非靶的比值（6.7±0.05）。这项研究的结果表明，[Tc]-表阿霉素可以作为成像和监测多药耐药金黄色葡萄球菌细菌感染治疗过程的选择。
