Flexibility-powered Pickering emulsion enhances mucus permeability to alleviate ulcerative colitis

Area of Science:

• Nanotechnology
• Materials Science
• Pharmacology

Background:

• Physicochemical properties of oral drug carriers impact intestinal interactions, in vivo fate, and efficacy.
• Pickering emulsions offer stability and advantages for enhancing bioavailability of encapsulated compounds.
• The role of Pickering emulsion flexibility in intestinal barrier interactions and delivery efficiency is not well understood.

Purpose of the Study:

• To develop a flexible Pickering emulsion (FPPE) for epigallocatechin gallate encapsulation.
• To investigate the mechanism of FPPE's flexible structure in mucus penetration, cellular uptake, and intestinal biodistribution.
• To evaluate the therapeutic efficacy of FPPE in an acute colitis mouse model.

Main Methods:

• Development of FPPE stabilized by chitosan nanoparticles.
• Assessment of mucus permeation, gastrointestinal retention, and drug absorption.
• In vitro studies on macrophage uptake, mitochondrial membrane potential, and reactive oxygen species.
• In vivo evaluation in a dextran sulfate sodium-induced acute colitis mouse model.

Main Results:

• FPPE demonstrated deformable adaptation for efficient mucus permeation and enhanced drug absorption.
• FPPE improved macrophage uptake, mitochondrial membrane potential, and triggered macrophage reprogramming.
• FPPE significantly alleviated intestinal inflammation and promoted barrier repair compared to rigid microspheres.

Conclusions:

• Pickering emulsion flexibility is crucial for facilitating intestinal mucus delivery and enhancing oral drug efficacy.
• FPPE offers a promising strategy for improving the delivery of encapsulated bioactive compounds.
• Understanding the role of flexibility can guide the future design and application of Pickering emulsions for drug delivery.