Radiolabeling, Quality Control, and Cell Binding Studies of New 99m Tc-Labeled Bisphosphonates: 99m Tc-Ibandronate Sodium

Turkish Journal of Pharmaceutical Sciences

article

Meliha EKİNCݹ  Derya İLEM ÖZDEMİR¹  Emre ÖZGENǹ  Evren GÜNDOĞDU¹  Makbule AŞIKOĞLU¹ 

[1]Ege University, Faculty of Pharmacy, Department of Radiopharmacy

关键词: Ibandronate sodium;    technetium-99m;    radiopharmaceuticals;    radiolabeling;    bone cancer cells;   

DOI  :  10.4274/tjps.galenos.2022.01346

来源: Galenos Yayinevi

【 摘 要 】

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 [99mTc] and quality control tests on the newly developed radiopharmaceutical ([99mTc]Tc-IBD) were performed using radioactive thin layer chromatography. After that, the incorporation of [99mTc]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 [99mTc]Tc-IBD with 200 μg.mL-1 IBD, 20 μg stannous chloride, and 99mTc 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 [99m95% [99mTc]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 [99mTc]Tc-IBD was -1.1014. The radiolabeled complex exhibited a higher rate of cell incorporation to U2OS cells compared to Reduced/Hydrolyzed 99mTcO4 -. 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.

【 授权许可】

Unknown