Radiolabeling and preclinical evaluation of technetium-99m labeled colistin

IF 1.6 3区工程技术 Q3 CHEMISTRY, INORGANIC & NUCLEAR Applied Radiation and Isotopes Pub Date : 2024-09-14 DOI:10.1016/j.apradiso.2024.111524

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Abstract

Introduction

Antibiotic resistance is a burden on the healthcare system. In present study, we have labeled an antibiotic named Colistimethate sodium (CMS) with technetium-99m (^99mTc) to develop a SPECT based imaging tracer.

Methods

We standardised the labeling using 0.5–2 mg of CMS (in water) using stannous chloride dihydrate as a reducing agent followed by addition of 370 ± 74 MBq of ^99mTc. A group of mice were injected intravenously (in tail vein) with 4–6 MBq of [^99mTc]Tc-CMS diluted with saline and euthanized at various time intervals. microSPECT Imaging (ϒ-eye) was acquired to study the biodistribution in the healthy mice.

Results

We standardised the labeling using 0.5 mg of colistin in 0.5 ml of saline with addition of 30 μg stannous chloride dihydrate. The retention factor value was 0.1–0.3 as compared to 0.9–1.0 for free ^99mTc by TLC and retention time was found to be 14.2 ± 1.3 min as evaluated by HPLC. The biodistribution data showed uptake in lungs, spleen, and liver at 30 min but the uptake decreased in lung at 60 min. The imaging data corroborated with the biodistribution data.

Conclusions

We could successfully label [^99mTc]Tc-CMS ^99mTc and we could study its biodistribution in healthy mice.

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锝-99m标记的可乐定的放射性标记和临床前评估

导言抗生素耐药性是医疗系统的负担。在本研究中，我们用锝-99m（99mTc）标记了一种名为考来烯胺酸钠（Colistimethate sodium，CMS）的抗生素，以开发一种基于 SPECT 的成像示踪剂。一组小鼠尾静脉注射 4-6 MBq 用生理盐水稀释的[99mTc]Tc-CMS，并在不同时间间隔内安乐死。采集 microSPECT 成像（ϒ-eye）以研究健康小鼠的生物分布。经 TLC 测定，保留因子值为 0.1-0.3，而游离 99mTc 的保留因子值为 0.9-1.0；经 HPLC 测定，保留时间为 14.2 ± 1.3 分钟。生物分布数据显示，30 分钟后肺部、脾脏和肝脏摄取99mTc，但 60 分钟后肺部摄取量下降。结论我们成功地标记了[99mTc]Tc-CMS 99mTc，并研究了它在健康小鼠体内的生物分布。

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来源期刊

Applied Radiation and Isotopes 工程技术-核科学技术

CiteScore

3.00

自引率

12.50%

发文量

406

审稿时长

13.5 months

期刊介绍： Applied Radiation and Isotopes provides a high quality medium for the publication of substantial, original and scientific and technological papers on the development and peaceful application of nuclear, radiation and radionuclide techniques in chemistry, physics, biochemistry, biology, medicine, security, engineering and in the earth, planetary and environmental sciences, all including dosimetry. Nuclear techniques are defined in the broadest sense and both experimental and theoretical papers are welcome. They include the development and use of α- and β-particles, X-rays and γ-rays, neutrons and other nuclear particles and radiations from all sources, including radionuclides, synchrotron sources, cyclotrons and reactors and from the natural environment. The journal aims to publish papers with significance to an international audience, containing substantial novelty and scientific impact. The Editors reserve the rights to reject, with or without external review, papers that do not meet these criteria. Papers dealing with radiation processing, i.e., where radiation is used to bring about a biological, chemical or physical change in a material, should be directed to our sister journal Radiation Physics and Chemistry.