Preclinical pharmacokinetics of radiolabelled hyaluronan

Pharmacol Rep. 2012;64(2):428-37. doi: 10.1016/s1734-1140(12)70784-3.

Abstract

Background: Hyaluronan (HYA) is a high molecular weight glucosaminoglycan with a great perspective for medical applications. Because HYA is widespread in the body, it is difficult to determine the fate of exogenously administered HYA.

Methods: In this study, HYAof different molecular weights (0.1-1 MDa) was labelled with (99m)Tc, and the distribution profiles were determined after administrating the HYA to rats.

Results: After the intravenous administration of (99m)Tc-HYA, a rapid decrease in the radioactivity of blood samples was observed, presumably because of (99m)Tc-HYA uptake by the liver; only minimal signs of liver radioactivity washout were detected. After the oral administration of (99m)Tc-HYA, no significant absorption to the central compartment was found. A preliminary study using (14)C-HYA exhibited a different distribution profile than (99m)Tc-HYA because of the different administered dose and the fate of the degradation products. Even with (14)C-HYA, only traces of radioactivity were absorbed after oral administration.

Conclusion: This paper provides quantitative information regarding the distribution parameters of radiolabelled HYA in preclinical experiments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Carbon Radioisotopes
  • Chromatography, Gel
  • Drug Evaluation, Preclinical
  • Drug Stability
  • Gastrointestinal Tract / metabolism
  • Hyaluronic Acid / blood
  • Hyaluronic Acid / chemistry
  • Hyaluronic Acid / pharmacokinetics*
  • Injections, Intravenous
  • Kidney / metabolism
  • Liver / metabolism
  • Male
  • Molecular Weight
  • Organ Specificity
  • Radiopharmaceuticals
  • Rats
  • Rats, Wistar
  • Sodium Pertechnetate Tc 99m
  • Tissue Distribution

Substances

  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Hyaluronic Acid
  • Sodium Pertechnetate Tc 99m