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Pharmaceuticals 2016, 9(3), 37; doi:10.3390/ph9030037

Strategies to Overcome Heparins’ Low Oral Bioavailability

1
Organic Chemistry and Pharmaceutical Laboratory, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
2
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR/CIMAR), University of Porto, Rua dos Bragas 289, 4050-123 Porto, Portugal
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 22 April 2016 / Revised: 15 June 2016 / Accepted: 23 June 2016 / Published: 29 June 2016
(This article belongs to the Special Issue Grand Celebration: 100th Anniversary of the Discovery of Heparin)
View Full-Text   |   Download PDF [1783 KB, uploaded 29 June 2016]   |  

Abstract

Even after a century, heparin is still the most effective anticoagulant available with few side effects. The poor oral absorption of heparins triggered the search for strategies to achieve oral bioavailability since this route has evident advantages over parenteral administration. Several approaches emerged, such as conjugation of heparins with bile acids and lipids, formulation with penetration enhancers, and encapsulation of heparins in micro and nanoparticles. Some of these strategies appear to have potential as good delivery systems to overcome heparin’s low oral bioavailability. Nevertheless, none have reached the market yet. Overall, this review aims to provide insights regarding the oral bioavailability of heparin. View Full-Text
Keywords: heparin; anticoagulant; oral bioavailability heparin; anticoagulant; oral bioavailability
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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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Neves, A.R.; Correia-da-Silva, M.; Sousa, E.; Pinto, M. Strategies to Overcome Heparins’ Low Oral Bioavailability. Pharmaceuticals 2016, 9, 37.

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