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%).
Highlights
Inflammation is part of the normal host response to infection and injury, excessive or inappropriate inflammation contributes to a range of acute and chronic human diseases which are characterized by the production of inflammatory cytokines, arachidonic acid–derived eicosanoids, other inflammatory agents and adhesion molecules [1]
Polymeric drug delivery systems (DDS) enhance the solubility of scarcely soluble drugs, improving their biodistribution and pharmacokinetics, and minimizing the side effects of the therapeutic molecules under study [33]
The therapeutic molecule RES has been loaded into amphiphilic NPs that have demonstrated a highly efficient encapsulation efficiency for other lipophilic drugs such as pyrene, pilocarpine and camptothecin [29,30,31,32]
Summary
Inflammation is part of the normal host response to infection and injury, excessive or inappropriate inflammation contributes to a range of acute and chronic human diseases which are characterized by the production of inflammatory cytokines, arachidonic acid–derived eicosanoids, other inflammatory agents and adhesion molecules [1]. High concentrations of Tumor necrosis factor (TNF-α), Interleukin-12 (IL-12), and Interleukin-6 (IL-6) are destructive and are implicated in some of the pathologic responses that occur in endotoxic shock, in acute respiratory distress syndrome, and in chronic inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease (IBD) [2]. The two most common forms of IBD are Crohn’s disease (CD) and ulcerative colitis (UC). They lead to long-term and sometimes irreversible impairment of gastro-intestinal structure and function [4]. In UC, a diffuse mucosal inflammation of the colon is mainly found as well as the coincident production of a complex mixture of inflammatory mediators
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