A Comparative Study of the Pharmacokinetics of Bis- and Pentaphosphonic Acids Labeled with Gallium-68 in Rats with Experimental Model of Bone Callus

Bull Exp Biol Med. 2020 Sep;169(5):644-647. doi: 10.1007/s10517-020-04945-z. Epub 2020 Sep 28.

Abstract

We analyzed biodistribution of 68Ga-labeled hydroxyethylidenediphosphonic acid (68Ga-HEDP) and diethylenetriaminepentakis(methylenephosphonic acid) (68Ga-DTPMP) in Wistar rats with experimental model of bone callus. It was shown that the content of 68Ga-DTPMP and 68Ga-HEDP in bone callus was ~1.5-fold higher than in intact femur. 68Ga-DTPMP was characterized by higher stability in vivo, higher uptake in the bone tissue, and lower uptake in others visceral organs in comparison with 68Ga-HEDP. Thus, 68Ga-DTPMP had more suitable pharmacokinetic properties than 68Ga-HEDP.

Keywords: bone callus; diethylenetriaminepentakis(methylenephosphonic acid); gallium-68; hydroxyethylidenediphosphonic acid.

MeSH terms

  • Animals
  • Bone and Bones / metabolism*
  • Bony Callus / metabolism*
  • Diphosphonates / metabolism
  • Diphosphonates / pharmacokinetics*
  • Disease Models, Animal
  • Gallium Radioisotopes / analysis*
  • Rats
  • Rats, Wistar

Substances

  • Diphosphonates
  • Gallium Radioisotopes
  • Gallium-68