Evaluation of carrier added and no carrier added 90Y-EDTMP as bone seeking therapeutic radiopharmaceutical

Pak J Pharm Sci. 2014 Jul;27(4):813-8.

Abstract

The optimum conditions to label ethylenediaminetetramethylene phosphonate (EDTMP) compound with (90)y as a potential candidate for bone metastases therapy were investigated. Yttrium-90 is a pure β-emitter and can be obtained by (89)y (n,γ) (90)y nuclear reaction in a reactor or from an in-house generator system ((90)sr(90)y). The preparation of (90)Y-EDTMPis described using (90)y, which was obtained from neutron irradiation of y2o3 as well as from a laboratory scale organic resin-based (90)sr--(90)y generator. Because of the radiolabeling yield of 90Y-EDTMP on ligand/metal molar ratio, incubation time and ph was evaluated. Under optimum parameters, the radiolabeling yields of (90)Y-EDTMP were <95% for no-carrier-added as well as carrier-added (90)y. The biodistribution of no-carrier-added and carrier-added (90)Y-EDTMP complexes in rats was identical. The results indicate that (90)y (carrier-added)-edtmp is also an effective bone pain palliation agent because of its rapid blood clearance, greater uptake in bones and little absorption in soft tissues.

MeSH terms

  • Animals
  • Bone Neoplasms / radiotherapy*
  • Bone Neoplasms / secondary
  • Drug Carriers
  • Isotope Labeling
  • Male
  • Organophosphorus Compounds / therapeutic use*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use*
  • Rats
  • Rats, Sprague-Dawley
  • Tissue Distribution
  • Yttrium Radioisotopes / therapeutic use*

Substances

  • Drug Carriers
  • Organophosphorus Compounds
  • Radiopharmaceuticals
  • Yttrium Radioisotopes
  • (ethylenedinitrilo)-tetramethylenephosphonic acid