Preclinical pharmacokinetics of radiolabelled hyaluronan.
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.


CONCLUSIONS
This paper provides quantitative information regarding the distribution parameters of radiolabelled HYA in preclinical experiments.
Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho 1203, CZ-500 05 Hradec Kralove, Czech Republic. Laznicek@faf.cuni.cz
Milan
M
Laznicek
Alice
A
Laznickova
Dagmar
D
Cozikova
Vladimir
V
Velebny
D000284:Administration, Oral; D000818:Animals; D002250:Carbon Radioisotopes; D002850:Chromatography, Gel; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D041981:Gastrointestinal Tract / Q000378:metabolism; D006820:Hyaluronic Acid / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008297:Male; D008970:Molecular Weight; D009928:Organ Specificity; D019275:Radiopharmaceuticals; D051381:Rats; D017208:Rats, Wistar; D013670:Sodium Pertechnetate Tc 99m; D014018:Tissue Distribution
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D006820:Hyaluronic Acid; D013670:Sodium Pertechnetate Tc 99m