Optimized Formulation of Sulfasalazine and Probiotic-Loaded Carrageenan Microparticles Using Design of Experiments...

Area of Science:

• Gastroenterology
• Pharmaceutics
• Biotechnology

Background:

• Ulcerative colitis (UC) is a chronic inflammatory bowel disease characterized by inflammation and epithelial barrier dysfunction.
• Sulfasalazine and probiotics show efficacy in UC, but combined colonic delivery is underexplored.
• Developing a targeted delivery system can enhance therapeutic effectiveness for UC.

Purpose of the Study:

• To develop and evaluate a colon-targeted microparticulate formulation containing sulfasalazine and a probiotic.
• To assess the synergistic anti-inflammatory effects and therapeutic potential for ulcerative colitis.

Main Methods:

• Microparticles were prepared using a Design of Experiments (DoE) approach.
• Co-encapsulation of probiotic to maintain viability during processing.
• In vitro (Caco-2 cells) and in vivo (acetic acid-induced colitis model) evaluations of epithelial integrity, inflammation, and tissue damage.

Main Results:

• Optimized microparticles demonstrated sustained sulfasalazine release and preserved probiotic viability.
• In vitro studies showed improved epithelial barrier function, reduced oxidative stress (ROS), and suppressed inflammatory markers (NF-κB).
• In vivo studies revealed significant reduction in colitis severity, improved tissue integrity, and better histopathological outcomes.

Conclusions:

• The combined sulfasalazine-probiotic microparticles offer a novel, dual-action approach for UC management.
• Probiotics enhanced gut barrier protection, while sustained sulfasalazine release provided localized therapeutic action.
• This synergistic formulation shows potential for enhanced anti-inflammatory efficacy and disease control in UC patients.