Electrosprayed 4-carboxybenzenesulfonamide-chitosan microspheres for acetazolamide delivery

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Biomedical Engineering

Background:

• Chitosan is a biocompatible polymer with potential for drug delivery.
• Developing effective drug carriers for acidic environments like the stomach remains a challenge.

Purpose of the Study:

• To synthesize and characterize 4-Carboxybenzensulfonamide-chitosan (4-CBS-chitosan) microspheres.
• To evaluate the drug loading and release properties of 4-CBS-chitosan microspheres using acetazolamide (ACZ) as a model drug.
• To assess the suitability of 4-CBS-chitosan microspheres as drug carriers in acidic conditions.

Main Methods:

• Electrospraying technique for microsphere preparation.
• Characterization using FTIR, DSC, SEM, and particle size analysis.
• Acetazolamide (ACZ) encapsulation efficiency and release studies in simulated gastric fluid (0.1N HCl; pH 1.2).

Main Results:

• 4-CBS-chitosan microspheres exhibited a high ACZ encapsulation efficiency of 90%, significantly higher than native chitosan (47%).
• Microspheres had a mean diameter of 3.1 μm with a low polydispersity index (0.4).
• ACZ-loaded 4-CBS-chitosan demonstrated sustained release (∼100% over 3h) compared to native chitosan (44% over 1.5h) in simulated gastric fluid.

Conclusions:

• 4-CBS-chitosan microspheres offer superior ACZ encapsulation and controlled release profiles in acidic media.
• The enhanced properties make 4-CBS-chitosan microspheres a viable drug delivery system for acidic environments, including the gastric mucosal wall.