Hishar Hassan and Muhamad Faiz Othman and Hairil Rashmizal Abdul Razak and Zainul Amiruddin Zakaria and Fathinul Fikri Ahmad Saad and Mohd Azuraidi Osman and Loh, Hui Yi and Zarif Ashhar and Jaleezah Idris and Mohd Hamdi Noor Abdul Hamid and Zaitulhusna M. Safee (2022) Preparation, optimisation, and in vitro evaluation of [¹⁸F] AlF-NOTA-Pamidronic acid for bone imaging PET. Molecules, 27. pp. 1-25.
![[img]](https://eprints.ums.edu.my/style/images/fileicons/text.png) |
Text
ABSTRACT.pdf Download (48kB) |
|
Text
FULL TEXT.pdf Restricted to Registered users only Download (4MB) |
Abstract
[¹⁸F] sodium fluoride ([¹⁸F] NaF) is recognised to be superior to [⁹⁹mTc]-methyl diphosphate ([⁹⁹mTc]Tc-MDP) and 2-deoxy-2-[¹⁸F]fluoro-D-glucose ([¹⁸F]FDG) in bone imaging. However, there is concern that [¹⁸F] NaF uptake is not cancer-specific, leading to a higher number of false-positive interpretations. Therefore, in this work, [¹⁸F] AlF-NOTA-pamidronic acid was prepared, optimised, and tested for its in vitro uptake. NOTA-pamidronic acid was prepared by an N-Hydroxysuccinimide (NHS) ester strategy and validated by liquid chromatography-mass spectrometry analysis (LCMS/MS). Radiolabeling of [¹⁸F] AlF-NOTA-pamidronic acid was optimised, and it was ensured that all quality control analysis requirements for the radiopharmaceuticals were met prior to the in vitro cell uptake studies. NOTA-pamidronic acid was successfully prepared and radiolabeled with ¹⁸F. The radiolabel was prepared in a 1:1 molar ratio of aluminium chloride (AlCl3) to NOTA-pamidronic acid and heated at 100 ◦C for 15 min in the presence of 50% ethanol (v/v), which proved to be optimal. The preliminary in vitro results of the binding of the hydroxyapatite showed that [¹⁸F] AlF-NOTApamidronic acid was as sensitive as [¹⁸F] sodium fluoride ([¹⁸F] NaF). Normal human osteoblast cell lines (hFOB 1.19) and human osteosarcoma cell lines (Saos-2) were used for the in vitro cellular uptake studies. It was found that [¹⁸F] NaF was higher in both cell lines, but [¹⁸F] AlF-NOTA-pamidronic acid showed promising cellular uptake in Saos-2. The preliminary results suggest that further preclinical studies of [¹⁸F] AlF-NOTA-pamidronic acid are needed before it is transferred to clinical research.
| Item Type: | Article |
|---|---|
| Keyword: | Aluminium fluorid, Al-F, Pamidronic acid, Radiopharmaceuticals, Radiochemistry, Positron emission tomography, Bone imaging |
| Subjects: | R Medicine > R Medicine (General) > R5-920 Medicine (General) R Medicine > RC Internal medicine > RC31-1245 Internal medicine > RC254-282 Neoplasms. Tumors. Oncology Including cancer and carcinogens |
| Department: | FACULTY > Faculty of Medicine and Health Sciences |
| Depositing User: | SITI AZIZAH BINTI IDRIS - |
| Date Deposited: | 16 Dec 2024 11:27 |
| Last Modified: | 16 Dec 2024 11:27 |
| URI: | https://eprints.ums.edu.my/id/eprint/42277 |
Actions (login required)
 |
View Item |