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Preparation, Characterization, and Radiolabeling of [ 68Ga]Ga-NODAGA-Pamidronic Acid: A Potential PET Bone Imaging Agent

Authors
  • Ashhar, Zarif1, 2
  • Yusof, Nor Azah1
  • Ahmad Saad, Fathinul Fikri3
  • Mohd Nor, Siti Mariam1
  • Mohammad, Faruq
  • Bahrin Wan Kamal, Wan Hamirul4
  • Hassan, Muhammad Hishar3
  • Ahmad Hassali, Hazlina4
  • Al-Lohedan, Hamad A.
  • 1 (S.M.M.N.)
  • 2 Pharmacy Department, National Cancer Institute, Putrajaya 62250, Malaysia
  • 3 (M.H.H.)
  • 4 (H.A.H.)
Type
Published Article
Journal
Molecules
Publisher
MDPI AG
Publication Date
Jun 09, 2020
Volume
25
Issue
11
Identifiers
DOI: 10.3390/molecules25112668
PMID: 32526838
PMCID: PMC7321328
Source
PubMed Central
Keywords
Disciplines
  • Article
License
Green

Abstract

Early diagnosis of bone metastases is crucial to prevent skeletal-related events, and for that, the non-invasive techniques to diagnose bone metastases that make use of image-guided radiopharmaceuticals are being employed as an alternative to traditional biopsies. Hence, in the present work, we tested the efficacy of a gallium-68 (68Ga)-based compound as a radiopharmaceutical agent towards the bone imaging in positron emitting tomography (PET). For that, we prepared, thoroughly characterized, and radiolabeled [68Ga]Ga-NODAGA-pamidronic acid radiopharmaceutical, a 68Ga precursor for PET bone cancer imaging applications. The preparation of NODAGA-pamidronic acid was performed via the N -Hydroxysuccinimide (NHS) ester strategy and was characterized using liquid chromatography-mass spectrometry (LC-MS) and tandem mass spectrometry (MSn). The unreacted NODAGA chelator was separated using the ion-suppression reverse phase-high performance liquid chromatography (RP-HPLC) method, and the freeze-dried NODAGA-pamidronic acid was radiolabeled with 68Ga. The radiolabeling condition was found to be most optimum at a pH ranging from 4 to 4.5 and a temperature of above 60 °C. From previous work, we found that the pamidronic acid itself has a good bone binding affinity. Moreover, from the analysis of the results, the ionic structure of radiolabeled [68Ga]Ga-NODAGA-pamidronic acid has the ability to improve the blood clearance and may exert good renal excretion, enhance the bone-to-background ratio, and consequently the final image quality. This was reflected by both the in vitro bone binding assay and in vivo animal biodistribution presented in this research.

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