Uptake of 153Sm-DTPA-bis-biotin and 99mTc-DTPA-bis-biotin in rat as-30D-hepatoma cells.
Labeled biotin has been used mainly for pretargeted therapy, an approach for increasing the amount of radioactivity delivered to a cancer cell. The aim of this investigation was to prepare (153)Sm-DTPA-bis-biotin and (99m)Tc-DTPA-bis-biotin in order to study their in vitro and in vivo uptake in rat AS-30D hepatoma cells found in ascites and in implanted tumor. DTPA-bis-biotin (pH 8) was (153)Sm labeled with (153)SmCl(3) and (99m)Tc-DTPA-bis-biotin was prepared via SnCl(2) reduction. Radiochemical purity was >98% in both cases. AS-30D hepatoma cells were obtained from ascites of a rat with hepatoma and were propagated in the peritoneum cavity of normal rats. In vitro ascites cell (153)Sm-DTPA-bis-biotin uptake was compared with (153)SmCl(3) cell uptake. The ratio cell (153)Sm-DTPA-bis-biotin/(153) SmCl(3) was 39.6 and when avidin was added it increased to 50. The ratio (99m)Tc-DTPA-bis-biotin/TcO(4)Na was 8.7. Concentration of (153)Sm-DTPA-bis-biotin in tumor 2, 3 and 24 h after administration, was 5, 15 and 3 times higher than in normal muscle (T/nT). Biodistribution in a 0.083-24 h time period showed that (153)Sm-DTPA-bis-biotin was taken up only by ascites tumor cells and hepatoma cells. Two and 3 h ratio ascites/liver (As/Lv) was 6.4 and 6.0. For (99m)Tc-DTPA-bis-biotin 2 and 3 h T/nT was 15.7 and 4.7 and 2 h As/Lv was 1.4. In conclusion, both radiopharmaceuticals show high uptake in rat AS-30D hepatoma cells in ascites and in implanted tumor. Since lung, thyroid, kidney, liver or pancreas carcinomas are ascites producing cancers (153)Sm-DTPA-bis-biotin would be an adequate therapeutic radiopharmaceutical for these patients whose life quality would be enhanced with control of ascites, and a reduction of the primary tumor and its metastases.
Correa-González
Luis
L
Servicio de Medicina Nuclear, Hospital de Especialidades, Instituto Mexicano del Seguro Social, Centro Médico Nacional Siglo XXI, Mexico.
Arteaga de Murphy
Consuelo
C
Ferro-Flores
Guillermina
G
Pedraza-López
Martha
M
Murphy-Stack
Eduardo
E
Mino-León
Dolores
D
Pérez-Villaseñor
Graciela
G
Díaz-Torres
Yaneth
Y
Muñóz-Olvera
Rodrigo
R
D000818:Animals; D001710:Biotin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D006528:Carcinoma, Hepatocellular / Q000000981:diagnostic imaging* / Q000378:metabolism* / Q000473:pathology; D005260:Female; D008113:Liver Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D009368:Neoplasm Transplantation; D009928:Organ Specificity; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D004369:Pentetic Acid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D012016:Reference Values; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
C400052:DTPA-bis-biotin; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C478095:technetium 99m DTPA-bisbiotin; D001710:Biotin; D004369:Pentetic Acid