Novel Natural Carrier‐Free Self‐Assembled Nanoparticles for Treatment of Ulcerative Colitis by Balancing Immune Microenvironment and Intestinal Barrier

Abstract

Ulcerative colitis (UC) is a chronic inflammatory illness affecting the colon and rectum, with current treatment methods being unable to meet the clinical needs of ulcerative colitis patients. Although nanomedicines are recognized as promising anti‐inflammatory medicines, their clinical application is limited by their high cost and unpredictable safety risks. In this study, we reveal that two natural phytochemicals, berberine (BBR) and hesperetin (HST), self‐assemble directly to form binary carrier‐free multi‐functional spherical nanoparticles (BBR‐HST NPs) through noncovalent bonds involving electrostatic interactions, π‐π stacking, and hydrogen bonding. Because of their synergistic anti‐inflammatory activity, berberine–hesperetin nanoparticles (BBR‐HST NPs) exhibits significantly better therapeutic effects on UC and inhibitory effects on inflammation than BBR and HST at the same dose by regulating the immune microenvironment and repairing the damaged intestinal barrier. Furthermore, BBR‐HST NPs exhibits good biocompatibility and biosafety. Thus, this study proves the potential of novel natural anti‐inflammatory nanoparticles as therapeutic agents for UC, which could promote the progress of drug development for UC and eventually benefit patients who suffering from it.This article is protected by copyright. All rights reserved

Collision of herbal medicine and nanotechnology: a bibliometric analysis of herbal nanoparticles from 2004 to 2023

“…Another study revealed that two natural plant compounds, berberine and hesperetin, directly self-assembled into carrier-free dual-function spherical berberine-hesperetin nanoparticles (BBR-HST NPs) through noncovalent bonds such as electrostatic interactions, π–π stacking, and hydrogen bonds. BBR-HST NPs exhibited synergistic anti-inflammatory effects, effectively modulating the immune environment and repairing damaged intestinal barriers, exhibiting significant advantages in the treatment of ulcerative colitis and inflammation as compared to equivalent doses of BBR and HST [ 88 ]. Furthermore, two natural compounds with antimicrobial and anti-inflammatory properties, berberine and sanguinarine, could self-assemble directly into carrier-free binary small molecule berberine-sanguinarine (BA-SAN) hydrogels through noncovalent bonds, such as electrostatic attraction, π–π stacking, and hydrogen bonding.…”