99mtc标记的头孢克肟用于感染的靶向成像:临床前评估和产后妇女的潜力。

Shahida Parveen, Rubaida Mehmood, Zara Jabeen, Kainat Warraich, Hafiza Samin Anjum, Daniyal Warraich, Mubashra Naz, Fatima Shams, Rida Sana
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引用次数: 0

摘要

靶向感染成像对产后妇女的准确诊断至关重要。该项目使用99mtc标记的头孢克肟开发一种放射性药物,用于检测、区分和治疗女性感染和脓肿。方法:与头孢克肟螯合的锝(TcO4-),经氯化亚锡还原,薄层色谱确证。小鼠注射标记化合物后,在1、2和3小时进行了热原性和稳定性测试。生物分布和SPECT (CT)成像显示注射后的体内方面。结果:用丙酮进行ITLC,显示头孢克肟与锝的结合率达到95%以上,具有较高的标记效率。标记的分子在三小时内保持稳定,提供了足够的成像窗口。扫描电镜分析证实了配合物上存在药物,红外光谱证实了头孢昔肟示踪剂键形成,HPLC定量了放射性标记收率。讨论:生物分布研究显示,放射性标记的头孢克肟主要积聚在肾脏和膀胱(31.38%)和肝脏(30.1%),表明肾脏和肝脏的清除途径。在小肠和大肠中出现中度摄取(24.6%),而在肺(4.3%)、心脏(4.1%)、胃和脾脏(5.4%)中分布较低。SPECT/CT成像显示药物积聚在感染的大腿组织中,将其与炎症部位区分开来,强调其在区分感染性和炎症性疾病方面的诊断潜力。该方法显示了在产后感染管理和超越临床翻译的希望。结论:用99mTc标记的头孢克肟可通过扫描准确检测啮齿动物感染。它的潜力可扩展到区分人体血浆中的健康细胞和恶性细胞,这表明在医疗诊断方面有希望,包括查明产后妇女不明病因的发热。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
99mTc-Labeled Cefixime for Targeted Imaging of Infections: Preclinical Evaluation and Potential in Postpartum Women.

Introduction: Targeted infection imaging is crucial for accurate diagnosis in postpartum women. This project uses 99mTc-labeled cefixime to develop a radiopharmaceutical for detecting, distinguishing, and treating infections and abscesses in women.

Method: Technetium (TcO4-) chelated with cefixime, reduced by stannous chloride, confirmed via thin-layer chromatography. Mice injected with the labeled compound showed pyrogenicity and stability tests at one, two, and three hours. Bio distribution and SPECT (CT) imaging revealed in vivo aspects post-injection.

Results: Radiolabeling achieved over 95% technetium binding to cefixime, as shown by ITLC with acetone, demonstrating high labeling efficiency. The labeled molecule remained stable for three hours, providing an adequate imaging window. SEM analysis confirmed drug presence on the complex, IR spectroscopy verified cefixime-tracer bond formation, and HPLC quantified radiolabeling yield.

Discussion: Bio distribution studies revealed that radiolabeled cefixime accumulated mainly in the kidney and bladder (31.38%) and liver (30.1%), indicating renal and hepatic clearance pathways. Moderate uptake appeared in the small and large intestines (24.6%), whereas lower distribution was observed in the lungs (4.3%), heart (4.1%), stomach, and spleen (5.4%). SPECT/CT imaging demonstrated drug accumulation in infected thigh tissues, distinguishing them from inflamed sites, underscoring its diagnostic potential for differentiating infectious from inflammatory conditions. The approach shows promise for clinical translation in postpartum infection management and beyond.

Conclusion: Cefixime, labeled with 99mTc, accurately detects rodent infections via scanning. Its potential extends to distinguishing healthy and malignant cells in human plasma, indicating promise in medical diagnostics, including identifying unknown-etiologic pyrexia in post-partum women.

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