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. 2019 Jan 18;20(2):398.
doi: 10.3390/ijms20020398.

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

Nieves Iglesias  1 , Elsa Galbis  2 , M Jesús Díaz-Blanco  3 , Ricardo Lucas  4 , Elena Benito  5 , M-Violante de-Paz  6
Affiliations

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

Nieves Iglesias et al. Int J Mol Sci. .

Abstract

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%).

Keywords: Crohn’s disease; IBD; colon; drug depot; hydrogels; inflammatory bowel disease; mucoadhesive; nanoparticles; ulcerative colitis.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
DALYs (disability-adjusted life years) per year of inflammatory bowel disease (IBD) in selected locations in 2017, ordered by incidence and sex.
Figure 2
Figure 2
Relative influence of the studied variables on encapsulation efficiency (EE%) in non-cross-linked and cross-linked nanoparticles.
Figure 3
Figure 3
Response surface for RES encapsulation efficiency percentage on both, non- and cross-linked NPs.
Figure 4
Figure 4
TGA traces of commercial chitosan (solid line) and the two RES-loaded CTS-NP composites.
Figure 5
Figure 5
SEM images of the loaded chitosan-based hydrogels: (A) Xr and (B) Non-Xr.
Figure 6
Figure 6
In vitro release profiles of resveratrol in simulated colon conditions from resveratrol-loaded NPs (A) and resveratrol-loaded CTS-NPs composites (B).
See this image and copyright information in PMC

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