Colon-targeted delivery of polyphenols: construction principles, targeting mechanisms and evaluation methods

AbstractPolyphenols have received considerable attention for their promotive effects on colonic health. However, polyphenols are mostly sensitive to harsh gastrointestinal environments, thus, must be protected. It is necessary to design and develop a colon-targeted delivery system to improve the stability, colon-targeting and bioavailability of polyphenols. This paper mainly introduces research on colon-targeted controlled release of polyphenols. The physiological features affecting the dissolution, release and absorption of polyphenol-loaded delivery systems in the colon are first discussed. Simultaneously, the types of colon-targeted carriers with different release mechanisms are described, and colon-targeting assessment models that have been studied so far and their advantages and limitations are summarized. Based on the current research on polyphenols colon-targeting, outlook and reflections are proposed, with the goal of inspiring strategic development of new colon-targeted therapeutics to ensure that the polyphenols reach the colon with complete bioactivity.Keywords: Colonic targetingpolyphenolscontrolled releaseconstruction principlesdelivery assessment Authors' contributionsYidi Wang: Conceptualization-Equal, Data curation-Equal, Investigation-Equal, Writing – original draft; Zhiying Li: Conceptualization-Equal, Data curation-Equal, Formal analysis; Yiwen Bao: Conceptualization-Equal, Investigation-Equal; Huijun Cui: Investigation-Equal, Project administration-Equal; Jiaxin Li: Investigation-Equal, Methodology-Equal; Xingyue Cui: Investigation-Equal, Resources-Equal; Mengzhu Wang: Investigation-Equal, Resources-Equal; Baoge Song: Methodology-Equal, Resources-Equal; Haikun Li: Methodology-Equal, Resources-Equal; Yi Chen: Resources-Equal, Supervision-Equal; WeiChen: Project administration-Equal, Resources-Equal; Shufang Yang: Investigation-Equal; Yiyun Yang: Project administration-Equal; Zhufeng Jin: Resources-Equal; Xu Si: Funding acquisition-Equal, Methodology-Equal, Software, Supervision-Equal, Validation, Writing – review & editing; Bin Li: Funding acquisition-Equal, Project administration-Equal, Resources-Equal, Supervision-Equal.Disclosure statementNo potential conflict of interest was reported by the author(s).Additional informationFundingThis work was supported by the National Natural Science Foundation of China [U21A20273], the Central Government-guided local Science and Technology development Fund Project [2023JH6/100500010] and the Scientific Research Funding Projects of Liaoning Province [LSNQN202010].