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Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release

In the present work, we demonstrate the preparation of chitosan-based composites as vehicles of the natural occurring multi-drug resveratrol (RES). Such systems are endowed with potential therapeutic effects on inflammatory bowel diseases (IBD), such as Crohn’s disease (CD) and ulcerative colitis, t...

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Autores principales: Iglesias, Nieves, Galbis, Elsa, Díaz-Blanco, M. Jesús, Lucas, Ricardo, Benito, Elena, de-Paz, M.-Violante
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359380/
https://www.ncbi.nlm.nih.gov/pubmed/30669264
http://dx.doi.org/10.3390/ijms20020398
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author Iglesias, Nieves
Galbis, Elsa
Díaz-Blanco, M. Jesús
Lucas, Ricardo
Benito, Elena
de-Paz, M.-Violante
author_facet Iglesias, Nieves
Galbis, Elsa
Díaz-Blanco, M. Jesús
Lucas, Ricardo
Benito, Elena
de-Paz, M.-Violante
author_sort Iglesias, Nieves
collection PubMed
description In the present work, we demonstrate the preparation of chitosan-based composites as vehicles of the natural occurring multi-drug resveratrol (RES). Such systems are endowed with potential therapeutic effects on inflammatory bowel diseases (IBD), such as Crohn’s disease (CD) and ulcerative colitis, through the sustained colonic release of RES from long-lasting mucoadhesive drug depots. The loading of RES into nanoparticles (NPs) was optimized regarding two independent variables: RES/polymer ratio, and temperature. Twenty experiments were carried out and a Box–Behnken experimental design was used to evaluate the significance of these independent variables related to encapsulation efficiency (EE). The enhanced RES EE values were achieved in 24 h at 39 °C and at RES/polymer ratio of 0.75:1 w/w. Sizes and polydispersities of the optimized NPs were studied by dynamic light scattering (DLS). Chitosan (CTS) dispersions containing the RES-loaded NPs were ionically gelled with tricarballylic acid to yield CTS-NPs composites. Macro- and microscopic features (morphology and porosity studied by SEM and spreadability), thermal stability (studied by TGA), and release kinetics of the RES-loaded CTS-NPs were investigated. Release patterns in simulated colon conditions for 48 h displayed significant differences between the NPs (final cumulative drug release: 79–81%), and the CTS-NPs composites (29–34%).
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spelling pubmed-63593802019-02-06 Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release Iglesias, Nieves Galbis, Elsa Díaz-Blanco, M. Jesús Lucas, Ricardo Benito, Elena de-Paz, M.-Violante Int J Mol Sci Article In the present work, we demonstrate the preparation of chitosan-based composites as vehicles of the natural occurring multi-drug resveratrol (RES). Such systems are endowed with potential therapeutic effects on inflammatory bowel diseases (IBD), such as Crohn’s disease (CD) and ulcerative colitis, through the sustained colonic release of RES from long-lasting mucoadhesive drug depots. The loading of RES into nanoparticles (NPs) was optimized regarding two independent variables: RES/polymer ratio, and temperature. Twenty experiments were carried out and a Box–Behnken experimental design was used to evaluate the significance of these independent variables related to encapsulation efficiency (EE). The enhanced RES EE values were achieved in 24 h at 39 °C and at RES/polymer ratio of 0.75:1 w/w. Sizes and polydispersities of the optimized NPs were studied by dynamic light scattering (DLS). Chitosan (CTS) dispersions containing the RES-loaded NPs were ionically gelled with tricarballylic acid to yield CTS-NPs composites. Macro- and microscopic features (morphology and porosity studied by SEM and spreadability), thermal stability (studied by TGA), and release kinetics of the RES-loaded CTS-NPs were investigated. Release patterns in simulated colon conditions for 48 h displayed significant differences between the NPs (final cumulative drug release: 79–81%), and the CTS-NPs composites (29–34%). MDPI 2019-01-18 /pmc/articles/PMC6359380/ /pubmed/30669264 http://dx.doi.org/10.3390/ijms20020398 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Iglesias, Nieves
Galbis, Elsa
Díaz-Blanco, M. Jesús
Lucas, Ricardo
Benito, Elena
de-Paz, M.-Violante
Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title_full Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title_fullStr Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title_full_unstemmed Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title_short Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
title_sort nanostructured chitosan-based biomaterials for sustained and colon-specific resveratrol release
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359380/
https://www.ncbi.nlm.nih.gov/pubmed/30669264
http://dx.doi.org/10.3390/ijms20020398
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