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Mar. Drugs 2018, 16(4), 132; https://doi.org/10.3390/md16040132

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

1
Saint-Petersburg Institute of Pharmacy, Leningrad Region, Vsevolozhsky District, Kuzmolovo P 245, 188663 Saint-Petersburg, Russia
2
RMC “House of Pharmacy”, Leningrad Region, Vsevolozhsky District, Zavodskaya str., 3, Kuzmolovo P 245, 188663 Saint-Petersburg, Russia
3
Federal State Budgetary Scientific Institution of Murmansk Marine Biological Institute, Kola Scientific Center of the Russian Academy of Sciences (MMBI KSC RAS), Vladimirskaya, 17, 183010 Murmansk, Russia
4
Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, P.O. Box 56 (Viikinkaari 5E), University of Helsinki, FI-00014 Helsinki, Finland
*
Author to whom correspondence should be addressed.
Received: 21 March 2018 / Revised: 5 April 2018 / Accepted: 16 April 2018 / Published: 18 April 2018
(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)
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Abstract

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 (AUC0–t = 10.74 µg·h/g; Cmax = 1.23 µg/g after 5 h), spleen (AUC0–t = 6.89 µg·h/g; Cmax = 0.78 µg/g after 3 h), and liver (AUC0–t = 3.26 µg·h/g; Cmax = 0.53 µg/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. View Full-Text
Keywords: anti-Xa activity; Fucus vesiculosus; fucoidan; kidneys; liver; pharmacokinetic; spleen anti-Xa activity; Fucus vesiculosus; fucoidan; kidneys; liver; pharmacokinetic; spleen
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Pozharitskaya, O.N.; Shikov, A.N.; Faustova, N.M.; Obluchinskaya, E.D.; Kosman, V.M.; Vuorela, H.; Makarov, V.G. Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats. Mar. Drugs 2018, 16, 132.

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