Biodistribution of 99mTc-HYNIC-lactadherin in mice--a potential tracer for visualizing apoptosis in vivo

Scand J Clin Lab Invest. 2010 Apr 19;70(3):209-16. doi: 10.3109/00365511003663648.

Abstract

Introduction: The aim of this study was to establish a radio synthesis of (99m)Tc-HYNIC-lactadherin for in vivo studies and to perform biodistribution analysis studies in mice, comparing (99m)Tc-HYNIC-lactadherin to (99m)Tc-HYNIC-annexin V.

Methods: The radiochemical purity of (99m)Tc-HYNIC-lactadherin was optimized by varying the amount of SnCl(2) in the synthesis. Furthermore, the need for bovine serum albumin (BSA) as a stabilizing agent was evaluated by following the stability by radiochemical purity measurement with and without the addition of BSA. A total of 24 mice were assigned to groups of 15 and nine mice, respectively. The animals were sacrificed at different time points; 10 min, 60 min, and 180 min.

Results: The synthesis of (99m)Tc-HYNIC-lactadherin for in vivo studies has been optimized to give a stable product without addition of BSA and with a radiochemical purity of more than 95%. Approximately 60% of the injected dose of (99m)Tc-HYNIC-lactadherin was found in the liver and 4-5% could be assigned to kidneys. In contrast, (99m)Tc-HYNIC-annexin V distributes with around 13% and 45% of the injected dose in liver and kidneys, respectively. Over the experimental period (10-180 min) only small distributional changes were observed for both probes.

Conclusion: In conclusion, the biodistribution of (99m)Tc-HYNIC-lactadherin, a potential new tracer for in vivo quantification of apoptosis, was evaluated. The small renal uptake of (99m)Tc-HYNIC-lactadherin makes it possible to image apoptosis in the kidneys, but the high liver clearance may be a disadvantage during myocardial perfusion.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Annexin A5 / pharmacokinetics
  • Apoptosis* / drug effects
  • Cattle
  • Electrophoresis, Polyacrylamide Gel
  • Etoposide / pharmacology
  • HL-60 Cells
  • Humans
  • Mice
  • Milk Proteins / pharmacokinetics*
  • Organotechnetium Compounds / pharmacokinetics*
  • Radioactive Tracers*
  • Time Factors
  • Tissue Distribution / drug effects

Substances

  • Annexin A5
  • Milk Proteins
  • Organotechnetium Compounds
  • Radioactive Tracers
  • technetium 99m HYNIC-bovine lactadherin
  • technetium Tc 99m HYNIC annexin V
  • Etoposide