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

Küçük Resim Yok

Tarih

2023

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Galenos Publ House

Erişim Hakkı

info:eu-repo/semantics/openAccess

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 [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 mu g.mL-1 IBD, 20 mu g 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 [99mTc]Tc-IBD was found to be greater than 95% at room temperature for up to 6 h. Additionally, chromatography analysis showed >95% [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.

Açıklama

Anahtar Kelimeler

Ibandronate sodium, technetium-99m, radiopharmaceuticals, radiolabeling, bone cancer cells, In-Vitro Evaluation, Bone-Seeking Agent, Biological Evaluation, Cancer, Ibandronate, Permeability

Kaynak

Turkish Journal of Pharmaceutical Sciences

WoS Q Değeri

Q3

Scopus Q Değeri

Q3

Cilt

20

Sayı

2

Künye