title: Preparation of 177Lu-labeled oxine in lipiodol as a possible agent for therapy of hepatocellular carcinoma: a preliminary animal study.
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.
authors.affiliation: Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
authors.forename: Suresh
authors.initials: S
authors.lastname: Subramanian
authors.forename: Tapas
authors.initials: T
authors.lastname: Das
authors.forename: Sudipta
authors.initials: S
authors.lastname: Chakraborty
authors.forename: Haladhar Dev
authors.initials: HD
authors.lastname: Sarma
authors.forename: Sharmila
authors.initials: S
authors.lastname: Banerjee
authors.forename: Grace
authors.initials: G
authors.lastname: Samuel
authors.forename: Meera
authors.initials: M
authors.lastname: Venkatesh
mesh_terms: D000818:Animals; D006528:Carcinoma, Hepatocellular / Q000139:chemically induced / Q000532:radiotherapy*; D004052:Diethylnitrosamine; D004353:Drug Evaluation, Preclinical; D004998:Ethiodized Oil / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D007459:Iodized Oil / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D007553:Isotope Labeling; D008114:Liver Neoplasms, Experimental / Q000139:chemically induced / Q000532:radiotherapy*; D008187:Lutetium / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D015125:Oxyquinoline / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011868:Radioisotopes / Q000493:pharmacokinetics / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: C555779:(177)Lu-oxine-lipiodol; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D004052:Diethylnitrosamine; D008187:Lutetium; D015125:Oxyquinoline; D007459:Iodized Oil; D004998:Ethiodized Oil