Colon Targeting pH-Responsive Coacervate Microdroplets for Treatment of Ulcerative Colitis.

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Gastroenterology

Background:

• Ulcerative colitis (UC) is a chronic inflammatory disease impacting quality of life and increasing colorectal cancer risk.
• Effective oral drug delivery and retention in colonic lesions remain significant challenges for UC treatment.
• Coacervate microdroplets offer potential for drug delivery due to facile fabrication and high drug loading.

Purpose of the Study:

• To develop a novel coacervate microdroplet system for targeted oral drug delivery in ulcerative colitis.
• To evaluate the stability, colon-targeting ability, and therapeutic efficacy of the developed system.

Main Methods:

• Fabrication of biocompatible diethylaminoethyl-dextran hydrochloride/sodium polyphenylene sulfonate coacervates coated with Eudragit S100 (EU-Coac).
• Loading of emodin into EU-Coac (EMO@EU-Coac) and assessment of its stability and pH-responsive release.
• In vivo evaluation of EMO@EU-Coac's colonic targeting, retention, and therapeutic effects on UC models.

Main Results:

• Developed EU-Coac demonstrated good stability in gastric conditions and pH-responsive release.
• EMO@EU-Coac effectively targeted and retained in the colon after oral administration.
• Treatment with EMO@EU-Coac attenuated inflammation, oxidative stress, repaired colonic epithelia, and balanced gut microbiota in UC models.

Conclusions:

• The developed EU-Coac system provides a novel and facile approach for targeted ulcerative colitis treatment.
• This coacervate microdroplet delivery system shows significant therapeutic potential for managing UC.
• The study highlights the promise of coacervate microdroplets in addressing challenges in oral drug delivery for gastrointestinal diseases.