{"title":"鼻内放射性碘化阿魏酸聚合胶束作为 ETRA 脑受体的首个核医学成像探针","authors":"Hend Fayez, Adli Selim, Rehab Shamma, Hassan Rashed","doi":"10.2174/0118744710269885231113070356","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.</p><p><strong>Material and methods: </strong>Ferulic acid (an ETRA antagonist) was radiolabeled using <sup>131</sup>I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of <sup>131</sup>I-ferulic acid after IN administration of <sup>131</sup>I-ferulic acid polymeric micelles, IN administration of <sup>131</sup>I-ferulic acid solution and IV administration of <sup>131</sup>I-ferulic acid solution.</p><p><strong>Results: </strong>Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. <sup>131</sup>I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N <sup>131</sup>I-ferulic acid polymeric micelles were greater than the two other routes at all periods.</p><p><strong>Conclusion: </strong>Our results provide <sup>131</sup>I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":"209-217"},"PeriodicalIF":1.5000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Intranasal Radioiodinated Ferulic Acid Polymeric Micelles as the First Nuclear Medicine Imaging Probe for ETRA Brain Receptor.\",\"authors\":\"Hend Fayez, Adli Selim, Rehab Shamma, Hassan Rashed\",\"doi\":\"10.2174/0118744710269885231113070356\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.</p><p><strong>Material and methods: </strong>Ferulic acid (an ETRA antagonist) was radiolabeled using <sup>131</sup>I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of <sup>131</sup>I-ferulic acid after IN administration of <sup>131</sup>I-ferulic acid polymeric micelles, IN administration of <sup>131</sup>I-ferulic acid solution and IV administration of <sup>131</sup>I-ferulic acid solution.</p><p><strong>Results: </strong>Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. <sup>131</sup>I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N <sup>131</sup>I-ferulic acid polymeric micelles were greater than the two other routes at all periods.</p><p><strong>Conclusion: </strong>Our results provide <sup>131</sup>I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.</p>\",\"PeriodicalId\":10991,\"journal\":{\"name\":\"Current radiopharmaceuticals\",\"volume\":\" \",\"pages\":\"209-217\"},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current radiopharmaceuticals\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2174/0118744710269885231113070356\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current radiopharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0118744710269885231113070356","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Intranasal Radioiodinated Ferulic Acid Polymeric Micelles as the First Nuclear Medicine Imaging Probe for ETRA Brain Receptor.
Introduction: The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.
Material and methods: Ferulic acid (an ETRA antagonist) was radiolabeled using 131I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of 131I-ferulic acid after IN administration of 131I-ferulic acid polymeric micelles, IN administration of 131I-ferulic acid solution and IV administration of 131I-ferulic acid solution.
Results: Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. 131I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N 131I-ferulic acid polymeric micelles were greater than the two other routes at all periods.
Conclusion: Our results provide 131I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.
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