RESUMEN
The aim of this study is to develop (177) Lu-5-Flourouracil as a potential cancer therapeutic radiopharmaceutical. 5-Flourouracil (5-FU) is widely accepted as an anticancer drug of broad spectrum fame. The labeling of 5-FU was carried out at different set of experimental conditions using high specific activity of (177) LuCl3 . The optimum conditions for maximum radiochemical yield was set: 5-FU (5 mg), (177) LuCl3 (185 MBq), diethylenetriaminepentaacetic acid (10 µg), reaction volume (2 mL), pH (5.5), temperature (80°C), and reaction time (20 min). The radiochemical labeling was assessed with Whatman No. 2 paper, instant thin layer chromatographic, and radio-HPLC, which revealed >94% labeling results with sufficient stability up to 6 h. Serum stability study also showed (177) Lu-5-FU promising stability. Biodistribution study in normal rats and rabbits showed liver, stomach, kidney, and heart as area of increased tracer accumulation just after injection, which decreased to 1.4%, 0.4%, 0.2%, and 0.39% ID/g, respectively, after 72 h. Glomerular filtration rate and cytotoxicity study results of (177) Lu-5-FU showed it had no adverse effect on renal function and nontoxic to blood cells. The promising characteristics of (177) Lu-5-FU, that is, clever elimination from kidney and nontoxic nature toward blood cells make it the radiopharmaceutical for further testing in patients for therapeutic purposes.
Asunto(s)
Fluorouracilo/síntesis química , Fluorouracilo/farmacocinética , Lutecio/uso terapéutico , Radioisótopos , Cintigrafía/métodos , Radiofármacos/síntesis química , Radiofármacos/farmacocinética , Animales , Estabilidad de Medicamentos , Fluorouracilo/química , Fluorouracilo/uso terapéutico , Semivida , Marcaje Isotópico , Masculino , Control de Calidad , Conejos , Radioquímica , Radiofármacos/química , Radiofármacos/uso terapéutico , Ratas , Ratas Sprague-Dawley , Distribución TisularRESUMEN
A complex of lincomycin was synthesized with technetium-99m. The synthesis was carried out by using SnCl2.2H2O as reducing agent and ascorbic acid as stabilizer. The effect of various parameters such as amount of ligand/reducing agent, pH value and reaction time on radio labeling process was studied. The characterization of the (99m)Tc-Lincomycin was performed by HPLC and electrophoresis Biodistribution studies were carried out by analyzing the model of bacterial infectious rats (Sprague-Dawley). The uptake of infectious lesions at different time interval was also studied by using scintigraphic technique. The complex showed effective target to non-target ratio for various inflammatory or infectious lesions. The (99m)Tc-Lincomycin effective binding to living bacteria and could be used successfully as an infection imaging agent.