Preparation and biodistribution of rhenium-188 ECD/Lipiodol in rats following hepatic arterial injection.
Radiolabeled Lipiodol has routinely been used in hepatoma therapy. In this article an attempt to develop a new (188)Re-ECD/Lipiodol radiopharmaceutical, in which the chelating agent ECD (ethyl cyteinate dimer), is the constituent of the known brain perfusion agent (99m)Tc-ECD, and an evaluation of its stability and biodistribution in rats with hepatic tumors is presented. First, (188)Re-ECD was prepared in a vial, followed by extraction with Lipiodol to get the final product, (188)Re-ECD/Lipiodol. The optimal labeling conditions for (188)Re-ECD were: (1) tartaric acid which is better than EDTA as a weak chelating agent; and (2) 15 mg of SnCl(2), as the reducing agent, and 5-10 mg of tartaric acid in each vial had a better labeling yield. The radiochemical purity of (188)Re-ECD/Lipiodol was more than 94%. Twenty-four male Sprague-Dawley rats with liver tumors were sacrificed at 1, 24, and 48 h (eight rats each time) after an injection of approximately 7.4 MBq of (188)Re-ECD/Lipiodol via the hepatic artery. The radioactivity in the liver tumor is significantly high following therapeutic arterial injection, and relatively low in other organs including the bone, spleen, brain, thyroid, stomach, muscle, blood, and testis throughout this study. In conclusion, the new preparation of (188)Re-ECD/Lipiodol is a candidate agent for the treatment of liver cancer.
Luo
Tsai-Yueh
TY
Chungtai Institute of Health Sciences and Technology, Taichung, Taiwan.
Hsieh
Bor-Tsung
BT
Wang
Shyh-Jen
SJ
Lin
Wan-Yu
WY
Lee
Te-Wei
TW
Shen
Lie-Hang
LH
Su
Ming-Jai
MJ
D000818:Animals; D004338:Drug Combinations; D006499:Hepatic Artery / Q000378:metabolism; D007269:Injections, Intra-Arterial; D007459:Iodized Oil / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000627:therapeutic use; D007553:Isotope Labeling / Q000379:methods; D008099:Liver / Q000378:metabolism*; D008113:Liver Neoplasms / Q000378:metabolism* / Q000532:radiotherapy; D008297:Male; D008657:Metabolic Clearance Rate; D009928:Organ Specificity; D009942:Organometallic Compounds / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D004338:Drug Combinations; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; C493916:rhenium-188 ethyl cysteinate dimer lipiodol; D007459:Iodized Oil