Radiolabeling and preclinical animal model evaluation of DTPA coupled 99mTc-labelled flutamide complex ([99mTc]DTPA-FLUT) as a potential radiotracer for cancer imaging.

IF 1.1 4区 医学 Q3 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Acta radiologica Pub Date : 2024-08-01 Epub Date: 2024-05-15 DOI:10.1177/02841851241249161
Syed Ali Raza Naqvi, Ahmad Junaid Hassan, Muhammad Ramzan Saeed Ashraf Janjua, Naseem Abbas, Ameer Fawad Zahoor, Sadaf Ul Hassan, Amjad Hussain
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Abstract

Background: Advances in molecular imaging strategies have had an effect on precise diagnosis and treatment. Research has been intensified to develop more effective and versatile radiopharmaceuticals to uplift diagnostic efficiency and, consequently, the treatment.

Purpose: To label the flutamide (FLUT) coupled with diethylenetriamine pentaacetate (DTPA) with technetium-99 m (99mTc) and to evaluate its binding efficiency with rhabdomyosarcoma (RMS) cancer cells.

Material and methods: Radiolabeling of FLUT with 185 MBq freshly eluted 99mTcO4-1 was carried out via DTPA bifunctional chelating agent using stannous chloride reducing agent at pH 5. The labeled compound was assessed for its purity using chromatography analysis, stability in saline and blood serum, AND charge using paper electrophoresis. Normal biodistribution was studied using a mouse model, while binding affinity with RMS cancer cells was studied using an internalization assay. The in vivo accumulation of RMS cancer cells in a rabbit model was monitored using a SPECT gamma camera.

Results: Radiolabeling reaction displayed a pharmaceutical yield of 97% and a stability assay showed >95% intact radiopharmaceutical up to 6 h in saline and blood serum. In vitro internalization studies showed the potential of [99mTc]DTPA-FLUT to enter into cancer cells. This biodistribution study showed rapid blood clearance and minimum uptake by body organs, and scintigraphy displayed the [99mTc]DTPA-FLUT uptake by lesion, induced by RMS cancer cell lines in rabbit.

Conclusion: Stable, newly developed [99mTc]DTPA-FLUT seeks its way to internalize into RMS cancer cells, indicating it could be a potential candidate for the diagnosis of RMS cancer.

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DTPA 偶联 99mTc 标记氟他胺复合物([99mTc]DTPA-FLUT)作为一种潜在的癌症成像放射性示踪剂的放射性标记和临床前动物模型评估。
背景:分子成像策略的进步对精确诊断和治疗产生了影响。目的:用锝-99 m (99mTc)标记氟他胺 (FLUT)和五乙酸二乙烯三胺 (DTPA),并评估其与横纹肌肉瘤 (RMS) 癌细胞的结合效率:在 pH 值为 5 的条件下,使用氯化亚锡还原剂,通过 DTPA 双功能螯合剂对 FLUT 进行 185 MBq 新鲜洗脱的 99mTcO4-1 放射性标记。利用小鼠模型研究了正常生物分布,同时利用内化试验研究了与 RMS 癌细胞的结合亲和力。使用 SPECT 伽玛相机监测了 RMS 癌细胞在兔子模型中的体内蓄积情况:结果:放射性标记反应的药物收率为97%,稳定性测定显示,在生理盐水和血清中6小时内,放射性药物的完整率大于95%。体外内化研究表明,[99mTc]DTPA-FLUT 有可能进入癌细胞。这项生物分布研究显示,[99mTc]DTPA-FLUT在血液中清除迅速,被身体器官摄取的量最少,闪烁成像显示,[99mTc]DTPA-FLUT被病变组织摄取,由兔RMS癌细胞株诱发:结论:新开发的稳定的[99mTc]DTPA-FLUT可内化到RMS癌细胞中,表明它可能成为诊断RMS癌的潜在候选物质。
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来源期刊
Acta radiologica
Acta radiologica 医学-核医学
CiteScore
2.70
自引率
0.00%
发文量
170
审稿时长
3-8 weeks
期刊介绍: Acta Radiologica publishes articles on all aspects of radiology, from clinical radiology to experimental work. It is known for articles based on experimental work and contrast media research, giving priority to scientific original papers. The distinguished international editorial board also invite review articles, short communications and technical and instrumental notes.
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