Rectally Administered Budesonide-Loaded Phase Transformable Premix Offers Improved Recovery of Intestinal Mucosa in...

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Biomedical Engineering

Background:

• Developing advanced drug delivery systems is crucial for treating inflammatory bowel diseases like ulcerative colitis.
• Liquid crystalline (LC) phases offer unique properties for controlled drug release and enhanced bioadhesion.
• Understanding the formation and characterization of novel LC structures is key to their therapeutic application.

Purpose of the Study:

• To investigate the water-induced formation of nonlamellar liquid crystalline structures from oleic acid, TPGS, and Transcutol P.
• To characterize the physicochemical and viscoelastic properties of the formed LC phases.
• To evaluate the efficacy of a budesonide-loaded LC formulation for treating ulcerative colitis in a mouse model.

Main Methods:

• Construction and analysis of pseudoternary phase diagrams.
• Characterization using polarized light microscopy and small-angle X-ray scattering (SAXS).
• Rheological testing (amplitude and frequency sweeps) and ex vivo bioadhesion studies.
• In vivo efficacy assessment in a mouse model of ulcerative colitis, including biochemical, histopathological, and Western blotting analyses.

Main Results:

• Nonlamellar liquid crystalline structures were successfully formed upon water addition.
• The LC phases exhibited viscoelastic properties and structural resilience.
• The budesonide-loaded LC formulation demonstrated significant therapeutic efficacy in alleviating ulcerative colitis symptoms and restoring colonic barrier function.
• The formulation suppressed the oxidative stress-inflammation axis and improved tight junction protein expression (occludin and ZO-1).

Conclusions:

• Water-induced formation of nonlamellar liquid crystals is feasible using oleic acid, TPGS, and Transcutol P.
• These LC formulations possess desirable properties for drug delivery, including bioadhesion and viscoelasticity.
• Rectal administration of budesonide-loaded LC formulation is an effective strategy for managing ulcerative colitis by modulating inflammation and enhancing barrier integrity.