Pardeep Kumar , Nagesh C Shanbhag# , Pradip Chaudhari , Bhabani Mohanty , Riptee Thakur , Gopalakrishnan M Sasidharan
{"title":"锝-99m标记的可乐定的放射性标记和临床前评估","authors":"Pardeep Kumar , Nagesh C Shanbhag# , Pradip Chaudhari , Bhabani Mohanty , Riptee Thakur , Gopalakrishnan M Sasidharan","doi":"10.1016/j.apradiso.2024.111524","DOIUrl":null,"url":null,"abstract":"<div><h3>Introduction</h3><p>Antibiotic resistance is a burden on the healthcare system. In present study, we have labeled an antibiotic named Colistimethate sodium (CMS) with technetium-99m (<sup>99m</sup>Tc) to develop a SPECT based imaging tracer.</p></div><div><h3>Methods</h3><p>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 <sup>99m</sup>Tc. A group of mice were injected intravenously (in tail vein) with 4–6 MBq of [<sup>99m</sup>Tc]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.</p></div><div><h3>Results</h3><p>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 <sup>99m</sup>Tc 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.</p></div><div><h3>Conclusions</h3><p>We could successfully label [<sup>99m</sup>Tc]Tc-CMS <sup>99m</sup>Tc and we could study its biodistribution in healthy mice.</p></div>","PeriodicalId":8096,"journal":{"name":"Applied Radiation and Isotopes","volume":"214 ","pages":"Article 111524"},"PeriodicalIF":1.6000,"publicationDate":"2024-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Radiolabeling and preclinical evaluation of technetium-99m labeled colistin\",\"authors\":\"Pardeep Kumar , Nagesh C Shanbhag# , Pradip Chaudhari , Bhabani Mohanty , Riptee Thakur , Gopalakrishnan M Sasidharan\",\"doi\":\"10.1016/j.apradiso.2024.111524\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Introduction</h3><p>Antibiotic resistance is a burden on the healthcare system. In present study, we have labeled an antibiotic named Colistimethate sodium (CMS) with technetium-99m (<sup>99m</sup>Tc) to develop a SPECT based imaging tracer.</p></div><div><h3>Methods</h3><p>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 <sup>99m</sup>Tc. A group of mice were injected intravenously (in tail vein) with 4–6 MBq of [<sup>99m</sup>Tc]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.</p></div><div><h3>Results</h3><p>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 <sup>99m</sup>Tc 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.</p></div><div><h3>Conclusions</h3><p>We could successfully label [<sup>99m</sup>Tc]Tc-CMS <sup>99m</sup>Tc and we could study its biodistribution in healthy mice.</p></div>\",\"PeriodicalId\":8096,\"journal\":{\"name\":\"Applied Radiation and Isotopes\",\"volume\":\"214 \",\"pages\":\"Article 111524\"},\"PeriodicalIF\":1.6000,\"publicationDate\":\"2024-09-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Applied Radiation and Isotopes\",\"FirstCategoryId\":\"5\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S096980432400352X\",\"RegionNum\":3,\"RegionCategory\":\"工程技术\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Applied Radiation and Isotopes","FirstCategoryId":"5","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S096980432400352X","RegionNum":3,"RegionCategory":"工程技术","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
Radiolabeling and preclinical evaluation of technetium-99m labeled colistin
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.
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.
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