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Mar. Drugs 2014, 12(11), 5677-5697; doi:10.3390/md12115677

Delivery of Berberine Using Chitosan/Fucoidan-Taurine Conjugate Nanoparticles for Treatment of Defective Intestinal Epithelial Tight Junction Barrier

Department of Chemical Engineering, Ming Chi University of Technology, New Taipei City 243, Taiwan
Department of Chemical and Materials Engineering, Tamkang University, New Taipei City 251, Taiwan
Department of Biochemistry and Molecular Cell Biology, School of medicine, Taipei Medical University, Taipei City 110, Taiwan
Graduate Institute of Medical Sciences, College of Medicine, Taipei Medical University, Taipei City 110, Taiwan
Author to whom correspondence should be addressed.
Received: 6 September 2014 / Revised: 31 October 2014 / Accepted: 13 November 2014 / Published: 24 November 2014
(This article belongs to the Special Issue Advances in Marine Chitin and Chitosan)
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Bacterial-derived lipopolysaccharides (LPS) can cause defective intestinal barrier function and play an important role in the development of inflammatory bowel disease. In this study, a nanocarrier based on chitosan and fucoidan was developed for oral delivery of berberine (Ber). A sulfonated fucoidan, fucoidan-taurine (FD-Tau) conjugate, was synthesized and characterized by Fourier transform infrared (FTIR) spectroscopy. The FD-Tau conjugate was self-assembled with berberine and chitosan (CS) to form Ber-loaded CS/FD-Tau complex nanoparticles with high drug loading efficiency. Berberine release from the nanoparticles had fast release in simulated intestinal fluid (SIF, pH 7.4), while the release was slow in simulated gastric fluid (SGF, pH 2.0). The effect of the berberine-loaded nanoparticles in protecting intestinal tight-junction barrier function against nitric oxide and inflammatory cytokines released from LPS-stimulated macrophage was evaluated by determining the transepithelial electrical resistance (TEER) and paracellular permeability of a model macromolecule fluorescein isothiocyanate-dextran (FITC-dextran) in a Caco-2 cells/RAW264.7 cells co-culture system. Inhibition of redistribution of tight junction ZO-1 protein by the nanoparticles was visualized using confocal laser scanning microscopy (CLSM). The results suggest that the nanoparticles may be useful for local delivery of berberine to ameliorate LPS-induced intestinal epithelia tight junction disruption, and that the released berberine can restore barrier function in inflammatory and injured intestinal epithelial. View Full-Text
Keywords: chitosan; fucoidan; nanoparticles; drug delivery; tight junction chitosan; fucoidan; nanoparticles; drug delivery; tight junction

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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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MDPI and ACS Style

Wu, S.-J.; Don, T.-M.; Lin, C.-W.; Mi, F.-L. Delivery of Berberine Using Chitosan/Fucoidan-Taurine Conjugate Nanoparticles for Treatment of Defective Intestinal Epithelial Tight Junction Barrier. Mar. Drugs 2014, 12, 5677-5697.

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