pH/ROS Dual-Sensitive Natural Polysaccharide Nanoparticles Enhance "One Stone Four Birds" Effect of Rhein on...

Area of Science:

• Biomaterials Science
• Nanotechnology
• Gastroenterology
• Pharmacology

Background:

• Ulcerative colitis (UC) is a chronic inflammatory condition with limited treatment options.
• Rhein (RH), a natural compound, shows potential for UC treatment due to anti-inflammatory and antioxidant properties.
• RH's therapeutic application is hindered by poor solubility, bioavailability, and colonic targeting.

Purpose of the Study:

• To develop a novel, pH/ROS-sensitive, mucoadhesive nanodelivery system for oral RH delivery.
• To evaluate the comprehensive therapeutic effects of RH-loaded nanoparticles (RH-F/C-NPs) for ulcerative colitis.

Main Methods:

• Fabrication of RH-F/C-NPs using a polyelectrolyte self-assembly method with chitosan (CS) and fucoidan (FU).
• Characterization of nanoparticle size, encapsulation efficiency, gastric stability, and colonic release.
• In vitro cellular uptake studies and in vivo evaluation in DSS-induced colitis models.

Main Results:

• RH-F/C-NPs exhibited optimal size (~233 nm) and high RH encapsulation rate (~94%).
• The nanoparticles demonstrated pH/ROS sensitivity for targeted colonic release and enhanced cellular uptake.
• In vivo studies showed significant reduction in DSS-induced colitis by RH-F/C-NPs, targeting inflammation, oxidative stress, barrier repair, and microflora regulation.

Conclusions:

• The developed polysaccharide-based nanodelivery system effectively overcomes RH's limitations for UC treatment.
• RH-F/C-NPs offer a multi-faceted therapeutic approach ('one stone four birds') for ulcerative colitis.
• This study presents a promising strategy for oral delivery of natural compounds for inflammatory bowel disease.