(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging
Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Huma...
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Veröffentlicht in: | Journal of labelled compounds & radiopharmaceuticals 2014-01, Vol.57 (1), p.36-41 |
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creator | Ïlem-Özdemir, Derya Asikoglu, Makbule Ozkilic, Hayal Yilmaz, Ferda Hosgor-Limoncu, Mine Ayhan, Semin |
description | Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by (99m) Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of (99m) Tc-DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of (99m) Tc-DOX make the new radiopharmaceutical valuable to examine for future studies. |
doi_str_mv | 10.1002/jlcr.3135 |
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Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by (99m) Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of (99m) Tc-DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of (99m) Tc-DOX make the new radiopharmaceutical valuable to examine for future studies.</description><identifier>EISSN: 1099-1344</identifier><identifier>DOI: 10.1002/jlcr.3135</identifier><identifier>PMID: 24259028</identifier><language>eng</language><publisher>England</publisher><subject>Animals ; Anti-Bacterial Agents - adverse effects ; Anti-Bacterial Agents - chemistry ; Anti-Bacterial Agents - pharmacokinetics ; Doxycycline - administration & dosage ; Doxycycline - chemistry ; Doxycycline - pharmacokinetics ; Drug Stability ; Escherichia coli Infections - diagnostic imaging ; Humans ; Isotope Labeling ; Radiochemistry ; Radionuclide Imaging ; Rats ; Rats, Wistar ; Technetium</subject><ispartof>Journal of labelled compounds & radiopharmaceuticals, 2014-01, Vol.57 (1), p.36-41</ispartof><rights>Copyright © 2013 John Wiley & Sons, Ltd.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,777,781,27905,27906</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24259028$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ïlem-Özdemir, Derya</creatorcontrib><creatorcontrib>Asikoglu, Makbule</creatorcontrib><creatorcontrib>Ozkilic, Hayal</creatorcontrib><creatorcontrib>Yilmaz, Ferda</creatorcontrib><creatorcontrib>Hosgor-Limoncu, Mine</creatorcontrib><creatorcontrib>Ayhan, Semin</creatorcontrib><title>(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging</title><title>Journal of labelled compounds & radiopharmaceuticals</title><addtitle>J Labelled Comp Radiopharm</addtitle><description>Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by (99m) Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of (99m) Tc-DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of (99m) Tc-DOX make the new radiopharmaceutical valuable to examine for future studies.</description><subject>Animals</subject><subject>Anti-Bacterial Agents - adverse effects</subject><subject>Anti-Bacterial Agents - chemistry</subject><subject>Anti-Bacterial Agents - pharmacokinetics</subject><subject>Doxycycline - administration & dosage</subject><subject>Doxycycline - chemistry</subject><subject>Doxycycline - pharmacokinetics</subject><subject>Drug Stability</subject><subject>Escherichia coli Infections - diagnostic imaging</subject><subject>Humans</subject><subject>Isotope Labeling</subject><subject>Radiochemistry</subject><subject>Radionuclide Imaging</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Technetium</subject><issn>1099-1344</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1kD1PwzAYhC0kREth4A8gj2VI8cebOGZD5VOqxFImhsh23hRXjlOcVNB_TyTK9Oik093pCLnibMEZE7fb4NJCcpmfkClnWmdcAkzIed9vGRs1wBmZCBC5ZqKcko-51u0NXbvsofs5uIMLPiL9HGkGvKOGRvymydS-C8ZiwJqaOHjru8E72nSJWuMGTN4E6mODbvBdpL41Gx83F-S0MaHHyyNn5P3pcb18yVZvz6_L-1W246IYMqEUNgBFLsocueQKDLfl2CZYU4O0ihusa9EwyQuwSkLDBUIBSipX2hzljMz_cnep-9pjP1St7x2GYCJ2-77ioEWhFBR6tF4frXvbYl3t0rg1Har_Q-QvNr9fDg</recordid><startdate>201401</startdate><enddate>201401</enddate><creator>Ïlem-Özdemir, Derya</creator><creator>Asikoglu, Makbule</creator><creator>Ozkilic, Hayal</creator><creator>Yilmaz, Ferda</creator><creator>Hosgor-Limoncu, Mine</creator><creator>Ayhan, Semin</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>201401</creationdate><title>(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging</title><author>Ïlem-Özdemir, Derya ; Asikoglu, Makbule ; Ozkilic, Hayal ; Yilmaz, Ferda ; Hosgor-Limoncu, Mine ; Ayhan, Semin</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p126t-277ef4465285e13174a1b8abe20fd43b71aedd2f03164b734f12e464737c8b5e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>Animals</topic><topic>Anti-Bacterial Agents - adverse effects</topic><topic>Anti-Bacterial Agents - chemistry</topic><topic>Anti-Bacterial Agents - pharmacokinetics</topic><topic>Doxycycline - administration & dosage</topic><topic>Doxycycline - chemistry</topic><topic>Doxycycline - pharmacokinetics</topic><topic>Drug Stability</topic><topic>Escherichia coli Infections - diagnostic imaging</topic><topic>Humans</topic><topic>Isotope Labeling</topic><topic>Radiochemistry</topic><topic>Radionuclide Imaging</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Technetium</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ïlem-Özdemir, Derya</creatorcontrib><creatorcontrib>Asikoglu, Makbule</creatorcontrib><creatorcontrib>Ozkilic, Hayal</creatorcontrib><creatorcontrib>Yilmaz, Ferda</creatorcontrib><creatorcontrib>Hosgor-Limoncu, Mine</creatorcontrib><creatorcontrib>Ayhan, Semin</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ïlem-Özdemir, Derya</au><au>Asikoglu, Makbule</au><au>Ozkilic, Hayal</au><au>Yilmaz, Ferda</au><au>Hosgor-Limoncu, Mine</au><au>Ayhan, Semin</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging</atitle><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle><addtitle>J Labelled Comp Radiopharm</addtitle><date>2014-01</date><risdate>2014</risdate><volume>57</volume><issue>1</issue><spage>36</spage><epage>41</epage><pages>36-41</pages><eissn>1099-1344</eissn><abstract>Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new (99m) Tc-labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by (99m) Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of (99m) Tc-DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of (99m) Tc-DOX make the new radiopharmaceutical valuable to examine for future studies.</abstract><cop>England</cop><pmid>24259028</pmid><doi>10.1002/jlcr.3135</doi><tpages>6</tpages></addata></record> |
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subjects | Animals Anti-Bacterial Agents - adverse effects Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacokinetics Doxycycline - administration & dosage Doxycycline - chemistry Doxycycline - pharmacokinetics Drug Stability Escherichia coli Infections - diagnostic imaging Humans Isotope Labeling Radiochemistry Radionuclide Imaging Rats Rats, Wistar Technetium |
title | (99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging |
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