{"title":"Preparation of 177Lu-labeled oxine in lipiodol as a possible agent for therapy of hepatocellular carcinoma: a preliminary animal study.","authors":"Suresh Subramanian, Tapas Das, Sudipta Chakraborty, Haladhar Dev Sarma, Sharmila Banerjee, Grace Samuel, Meera Venkatesh","doi":"10.1089/cbr.2010.0792","DOIUrl":null,"url":null,"abstract":"<p><p>Hepatocellular carcinoma (HCC) is one of the most prevalent forms of cancer with high morbidity. (131)I-lipiodol is used clinically and has been found to be effective for the treatment of HCC. However, this preparation has its limitations, including compromised yield and stability of exchange labeling and unnecessary dose burden from gamma emissions. In the present study, (177)Lu-oxine in lipiodol was considered as a possible alternative for radioiodinated lipiodol. Oxine or 8-hydroxyquinoline was labeled with (177)Lu obtained by neutron irradiation of natural lutetium. Under optimized conditions, the radiolabeled complex was obtained with yields >98% and adequate in vitro stability. (177)Lu-oxine dispersed in lipiodol showed appreciable uptake into rat liver cells (normal and HCC-induced) in vitro. (177)Lu-oxine-lipiodol showed initial localization in the liver, but subsequent leakage of radioactivity with deposition in the skeletal tissue was seen. The studies suggest that (177)Lu-oxine dispersed in lipiodol might not be suitable for treatment of HCC.</p>","PeriodicalId":518937,"journal":{"name":"Cancer biotherapy & radiopharmaceuticals","volume":" ","pages":"539-43"},"PeriodicalIF":0.0000,"publicationDate":"2010-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1089/cbr.2010.0792","citationCount":"18","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Cancer biotherapy & radiopharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1089/cbr.2010.0792","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2010/9/19 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 18
Abstract
Hepatocellular carcinoma (HCC) is one of the most prevalent forms of cancer with high morbidity. (131)I-lipiodol is used clinically and has been found to be effective for the treatment of HCC. However, this preparation has its limitations, including compromised yield and stability of exchange labeling and unnecessary dose burden from gamma emissions. In the present study, (177)Lu-oxine in lipiodol was considered as a possible alternative for radioiodinated lipiodol. Oxine or 8-hydroxyquinoline was labeled with (177)Lu obtained by neutron irradiation of natural lutetium. Under optimized conditions, the radiolabeled complex was obtained with yields >98% and adequate in vitro stability. (177)Lu-oxine dispersed in lipiodol showed appreciable uptake into rat liver cells (normal and HCC-induced) in vitro. (177)Lu-oxine-lipiodol showed initial localization in the liver, but subsequent leakage of radioactivity with deposition in the skeletal tissue was seen. The studies suggest that (177)Lu-oxine dispersed in lipiodol might not be suitable for treatment of HCC.
肝细胞癌(HCC)是最常见的癌症之一,发病率高。(131) i -脂醇已被临床应用,并被发现对HCC的治疗有效。然而,这种制备有其局限性,包括交换标记的产率和稳定性受损以及伽马辐射带来的不必要的剂量负担。在本研究中,(177)脂醇中的卢氧被认为是放射性碘化脂醇的可能替代品。用天然镥中子辐照得到的(177)Lu标记氧或8-羟基喹啉。在优化条件下,得到的放射性标记配合物收率>98%,体外稳定性良好。(177)在体外实验中,分散在脂醇中的Lu-oxine被正常和hcc诱导的大鼠肝细胞明显摄取。(177)卢氧-脂醇最初定位于肝脏,但随后放射性泄漏并沉积在骨骼组织中。研究提示(177)分散在脂醇中的卢氧可能不适合治疗HCC。