Rational Design of Polyphenol-Poloxamer Nanovesicles for Targeting Inflammatory Bowel Disease Therapy

Abstract

Currently, there is no curative treatment for inflammatory bowel disease (IBD), which has an increased risk of colitis-associated cancer. Corticosteroids are the main clinical IBD therapeutics but have significant side effects. Even heavy corticosteroid use can result in the failure of IBD treatment which may lead to resective surgery. In this study, we designed one type of new drug-delivery system (DDS) delivering dexamethasone (DEX), an anti-inflammation corticosteroid, for IBD therapy. This DDS was screened by hydrogen-bonding-induced facile self-assembly of natural and safe polyphenols and polymers. The nanoparticles fabricated from tannic acid and Pluronic F-68 have a uniform spherical shape. With approximately 10% DEX loaded, PPNP-DEX showed responsive release behavior in the presence of esterase. Moreover, PPNP-DEX exhibited great potential in radical scavenging at inflammation sites. Drug retention rates can also be enhanced in mice with colitis compared with healthy controls because of this inflammation targeting ability. Owing to all these advantages, PPNP-DEX achieved remarkable treatment efficacy in colitis mice compared with PPNP or free DEX. This study demonstrates PPNP as a promising drug-delivery platform for IBD therapy. More importantly, it provides a new design strategy of therapeutics for various inflammatory diseases.