Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats

• Published in: Marine Drugs
• Main Authors: Pozharitskaya, Olga N., Shikov, Alexander N., Faustova, Natalya M., Obluchinskaya, Ekaterina D., Kosman, Vera M., Vuorela, Heikki, Makarov, Valery G.
• Other Authors: Faculty of Pharmacy, Division of Pharmaceutical Biosciences, Pharmaceutical Design and Discovery group, Drug Research Program
• Format: Article in Journal/Newspaper
• Language: English
• Published: MDPI 2018
• Subjects: anti-Xa activity; Fucus vesiculosus; fucoidan; kidneys; liver; pharmacokinetic; spleen; MOLECULAR-WEIGHT; SULFATED POLYSACCHARIDES; UNFRACTIONATED HEPARIN; BROWN SEAWEEDS; HUMAN PLASMA; ANTICOAGULANT; OSTEOARTHRITIS; ENOXAPARIN; ANTIBODY; EXTRACT; 317 Pharmacy; Greenland; Pacific
• Online Access: http://hdl.handle.net/10138/235213

Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in Fucus (F.) vesiculosus. The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from F. vesiculosus. The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC(0-t) = 10.74 mu g.h/g; C-max = 1.23 mu g/g after 5 h), spleen (AUC(0-t) = 6.89 mu g.h/g; C-max = 0.78 mu g/g after 3 h), and liver (AUC(0-t) = 3.26 mu g.h/g; C-max = 0.53 mu g/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan. Peer reviewed