Radiolabeling, Quality Control, and Cell Binding Studies of New 99mTc-Labeled Bisphosphonates: 99mTc-Ibandronate Sodium
Makaleler > Tam Makale · 2022
Yazarlar: Meliha EKİNCİ, Derya İLEM ÖZDEMİR, Emre ÖZGENÇ, Evren ATLIHAN GÜNDOĞDU, MAKBULE AŞIKOĞLU
Turkish Journal of Pharmaceutical Sciences, Diğer Kurumların Hakemli Dergileri, Uluslararası, Scopus, 2022, cilt 20, ss 91-99
DOI: 10.4274/tjps.galenos.2022.01346
Özet
Objectives: Early detection of bone cancer is critical for treating symptoms, minimizing pain, and increasing overall quality of life.It is critical to develop novel radiopharmaceuticals with high labeling efficiency and stability for the diagnosis of bone cancer.This research aims to design a novel radiopharmaceutical that may be used to diagnose bone cancer.Materials and Methods: In this study, ibandronate sodium (IBD), a bisphosphonate analog, was radiolabeled with technetium-99m [ 99m Tc] and quality control tests on the newly developed radiopharmaceutical ([ 99m Tc]Tc-IBD) were performed using radioactive thin layer chromatography.After that, the incorporation of [ 99m Tc]Tc-IBD into hydroxyapatite (HA) crystals and a human bone osteosarcoma cell line (U2OS) was tested.Results: According to the results obtained, optimal radiolabeling procedure was obtained for [ 99m Tc]Tc-IBD with 200 µg.mL-1 IBD, 20 µg stannous chloride, and 99m Tc with 37 MBq radioactivity.The reaction mixture was adjusted to pH 5.5 and incubated at room temperature for 15 min.The radiochemical purity of [ 99m Tc]Tc-IBD was found to be greater than 95% at room temperature for up to 6 h.Additionally, chromatography analysis showed >95% [ 99m Tc]Tc-IBD complex formation with promising stability for up to 24 h in saline and up to 2 h in cell medium.The percentage binding of IBD to HA was 83.70 ± 3.67 and the logP of [ 99m Tc]Tc-IBD was -1.1014.The radiolabeled complex exhibited a higher rate of cell incorporation to U2OS cells compared to Reduced/Hydrolyzed 99m TcO 4 -. Conclusion:The newly produced radiopharmaceutical is very promising according to the results of in vitro cell culture, HA binding, and quality studies, and will be a step forward for further studies in nuclear medicine for bone cancer diagnostics.