Chitosan-based oral colon-specific delivery systems for polyphenols: recent advances and emerging trends

Oral colon-targeted delivery systems (OCDSs) have attracted great attention in the delivery of active compounds targeted to the colon for the treatment of colon and non-colon diseases with the advantages of enhanced efficacy and reduced side effects. Chitosan, the second-most abundant biopolymer next to cellulose, has great biocompatibility, is non-toxic, is sensitive to colonic flora and shows strong adhesion to colonic mucus, making it an ideal biomaterial candidate for the construction of OCDSs. Being rich in functional groups, the chitosan structure is easily modified, both physically and chemically, for the fabrication of delivery systems with diverse geometries, including nanoparticles, microspheres/microparticles, and hydrogels, that are resistant to the harsh environment of the upper gastrointestinal tract (GIT). This review offers a detailed overview of the preparation of chitosan-based delivery systems as the basis for building OCDSs. A variety of natural polyphenols with potent biological activities are used to treat diseases of the colon, or to be metabolized as active ingredients by colonic microorganisms to intervene in remote organ diseases after absorption into the circulation. However, the poor solubility of polyphenols limits their application, and the acidic environment of the upper GIT and various enzymes in the small intestine disrupt their structure and activity. As a result, the development of OCDSs for polyphenols has become an emerging and popular area of current research in the past decade. Thus, the second objective of this review is to systematically summarize the most recent research findings in this area and shed light on the future development of chitosan-based OCDSs for nutritional and biomedical applications.