Radiation Physics and Engineering
A peer-reviewed journal published by K. N. Toosi University of Technology

Comparison of radiolabeled bisphosphonates in bone metastasis

Document Type : Research Article

Authors

Mostafa Erfani
Azadeh Mikaeili
Mostafa Goudarzi
Zhila Fallah
Maryam Rezaei

Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran

https://doi.org/10.22034/rpe.2024.467196.1204
Abstract
Bisphosphonates have a very high affinity for bone minerals because they bind to hydroxyapatite crystals. Based on this fact, it was hypothesized to evaluate bone uptake for 99mTc/188Re radiolabeled bisphosphonates to determine the order of uptake in the bone as agents for imaging or treatment of skeletal disorders. Radiolabeling of bisphosphonate samples were performed by adding 185 MBq of 99mTc/188Re in saline, and SnCl2, 2H2O and ascorbic acid as reducing agents. Radioactive thin layer chromatography (RTLC) was used to determine the radiochemical purity. The stability of radiocomplexes was investigated in saline and human serum. Bone uptake was evaluated through biodistribution experiments in normal mice. A radiochemical purity of >90% was obtained for evaluated radiotracers. Bone accumulation and rapid renal excretion were observed in the biological assessment of all evaluated bisphosphonates at 2 hours post injection. Although bone uptake was desirable for investigated bisphosphonates, it appears that third-generation bisphosphonates can be used as novel bone imaging or therapeutic agents.

Highlights

  • New generations of bisphosphonate tracers have been developed.
  • Prepared conjugate showed high labeling yields and specific activity.
  • The tracers were stable in saline solution.
  • High bone uptake followed by low liver uptake are obtained at early time point and for third generation bisphosphonate.

Keywords

99mTc/188Re
Radiochemical yield
Biodistribution
Imaging
 
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Radiation Physics and Engineering
Volume 6, Issue 2
Winter 2025
Pages 41-46

  • Receive Date 10 July 2024
  • Revise Date 15 November 2024
  • Accept Date 12 November 2024

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