Colon Targeting pH ‐Responsive Coacervate Microdroplets for Treatment of Ulcerative Colitis

A biocompatible coacervate microdroplets, which loaded emodin and coated with eudragit S100 (EMO@EU-Coac) can achieve stability in gastric acid after oral administration and targets colon lesions. And EMO@EU-Coac can achieve effective treatment of UC through anti-inflammation, anti-oxidative stress, repair of the intestinal epithelial barrier, and regulation of intestinal microbiota balance. AbstractUlcerative colitis (UC), an immune-mediated chronic inflammatory disease, drastically impacts patients' quality of life and increases their risk of colorectal cancer worldwide. However, effective oral targeted delivery and retention of drugs in colonic lesions are still great challenges in the treatment of UC. Coacervate microdroplets, formed by liquid –liquid phase separation, are recently explored in drug delivery as the simplicity in fabrication, spontaneous enrichment on small molecules and biological macromolecules, and high drug loading capacity. Herein, in this study, a biocompatible diethylaminoethyl-dextran hydrochloride/sodium polyphen ylene sulfonate coacervates, coated with eudragit S100 to improve the stability and colon targeting ability, named EU-Coac, is developed. Emodin, an active ingredient in traditional Chinese herbs proven to alleviate UC symptoms, is loaded in EU-Coac (EMO@EU-Coac) showing good stability in gastric ac id and pepsin and pH-responsive release behavior. After oral administration, EMO@EU-Coac can effectively target and retain in the colon, dis...
Source: Small - Category: Nanotechnology Authors: Tags: Research Article Source Type: research