The Pharmacokinetics of Fucoidan after Topical Application to Rats

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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.

Title: The Pharmacokinetics of Fucoidan after Topical Application to Rats
Author: Pozharitskaya, Olga N.; Shikov, Alexander N.; Obluchinskaya, Ekaterina D.; Vuorela, Heikki
Publisher: Multidisciplinary Digital Publishing Institute
Date: 2019-12-06
Abstract: Fucoidan, a fucose-rich polysaccharide from brown algae, has been used for transdermal<br />formulations targeting inflammatory skin conditions, for the treatment of thrombosis, vascular<br />permeability diseases, subcutaneous wounds, and burns. However, the pharmacokinetics of<br />fucoidan after topical application has not been described. In this study, an ointment (OF)<br />containing 15% fucoidan was topically applied to rats at the doses of 50&ndash;150 mg/g. The anti-Xa<br />activity was selected as the biomarker, and the amidolytic assay method was validated and applied<br />for pharmacokinetic studies of fucoidan. Fucoidan in OF penetrated the skin and distributed into<br />the skin, striated muscle, and plasma with AUC0&ndash;48 = 0.94 &mu;g&middot;h/g, 2.22 &mu;g&middot;h/g, and 1.92 &mu;g&middot;h/mL,<br />respectively. The longest half-life for fucoidan was observed in plasma, then in striated muscle and<br />skin. It was found that the pharmacokinetics of fucoidan after topical OF application was linear, in<br />the range of 50&ndash;150 mg/kg. No accumulation of fucoidan in plasma was observed after repeated<br />topical applications of 100 mg/kg during five days. Our results support the rationality of topical<br />application of formulations with fucoidan.

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