Novel self-assembled mesalamine-sucralfate complexes: preparation, characterization, and formulation aspects

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery Systems

Background:

• Mesalamine (MES) is an anti-inflammatory agent, and sucralfate (SUC) possesses bioadhesive and mucosal healing properties.
• Ulcerative colitis treatment could benefit from a fixed-dose combination leveraging these complementary actions.

Purpose of the Study:

• To investigate the self-assembly and complex formation between mesalamine and sucralfate.
• To develop a novel fixed-dose combination product for improved ulcerative colitis therapy.

Main Methods:

• Spray-drying was employed to co-process mesalamine and sucralfate at various ratios (25:75, 50:50, 75:25).
• Structural characterization utilized X-Ray, FTIR, SEM, DSC, and (1)H NMR to analyze the formed complexes.
• In vitro studies assessed the release profile of mesalamine from the developed oral solid dosage forms.

Main Results:

• Structural analyses confirmed the interaction and self-assembly between MES and SUC, forming a new entity with distinct properties.
• (1)H NMR indicated complexation occurred in aqueous suspension prior to spray-drying, driven by drug-drug self-assembling.
• In vitro testing demonstrated controlled mesalamine release from MES-SUC complexes, indicating potential for colon targeting.

Conclusions:

• Co-processing mesalamine and sucralfate via spray-drying is an effective method for creating novel self-assembled compounds.
• The developed MES-SUC complexes offer a promising foundation for new colon-targeted delivery systems.
• This research opens avenues for a new class of compounds for inflammatory bowel disease treatment.