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Open AccessArticle

The Pharmacokinetics of Fucoidan after Topical Application to Rats

1
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
2
St. Petersburg State Chemical Pharmaceutical University, Prof. Popov, 14, 197376 Saint-Petersburg, Russia
3
Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5E), FI-00014 Helsinki, Finland
*
Author to whom correspondence should be addressed.
Mar. Drugs 2019, 17(12), 687; https://doi.org/10.3390/md17120687
Received: 15 November 2019 / Revised: 30 November 2019 / Accepted: 5 December 2019 / Published: 6 December 2019
(This article belongs to the Special Issue Pharmacokinetic Research of Marine Drugs)
Fucoidan, a fucose-rich polysaccharide from brown algae, has been used for transdermal formulations targeting inflammatory skin conditions, for the treatment of thrombosis, vascular permeability diseases, subcutaneous wounds, and burns. However, the pharmacokinetics of fucoidan after topical application has not been described. In this study, an ointment (OF) containing 15% fucoidan was topically applied to rats at the doses of 50–150 mg/g. The anti-Xa activity was selected as the biomarker, and the amidolytic assay method was validated and applied for pharmacokinetic studies of fucoidan. Fucoidan in OF penetrated the skin and distributed into the skin, striated muscle, and plasma with AUC0–48 = 0.94 μg·h/g, 2.22 μg·h/g, and 1.92 µg·h/mL, respectively. The longest half-life for fucoidan was observed in plasma, then in striated muscle and skin. It was found that the pharmacokinetics of fucoidan after topical OF application was linear, in the range of 50–150 mg/kg. No accumulation of fucoidan in plasma was observed after repeated topical applications of 100 mg/kg during five days. Our results support the rationality of topical application of formulations with fucoidan. View Full-Text
Keywords: fucoidan; topical application; pharmacokinetics; ointment; skin; striated muscle fucoidan; topical application; pharmacokinetics; ointment; skin; striated muscle
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MDPI and ACS Style

Pozharitskaya, O.N.; Shikov, A.N.; Obluchinskaya, E.D.; Vuorela, H. The Pharmacokinetics of Fucoidan after Topical Application to Rats. Mar. Drugs 2019, 17, 687.

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