Mucoadhesive microspheres containing anti-hypertensive agent: formulation and characterization

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biomaterials

Background:

• Mucoadhesive drug delivery systems enhance therapeutic efficacy by prolonging drug residence time at absorption sites.
• Furosemide, a diuretic, requires effective delivery strategies to optimize its therapeutic outcomes.
• Sodium alginate, HPMC E50, and sodium CMC are biocompatible polymers suitable for microsphere formulation.

Purpose of the Study:

• To formulate and characterize furosemide-loaded mucoadhesive microspheres using sodium alginate and mucoadhesive polymers.
• To investigate the effect of mucoadhesive polymers on drug release kinetics and mucoadhesion properties.
• To evaluate the potential of these microspheres as a controlled drug delivery system.

Main Methods:

• Mucoadhesive microspheres were prepared using the ionic gelation technique with sodium alginate, furosemide, and varying ratios of HPMC E50 or sodium CMC.
• Calcium chloride was employed as a crosslinking agent to control drug release.
• Microsphere characterization included production yield, particle size analysis, encapsulation efficiency, mucoadhesion testing, and in vitro dissolution studies.
• Differential Scanning Calorimetry (DSC) and Scanning Electron Microscopy (SEM) were utilized for formulation analysis.

Main Results:

• The prepared microspheres exhibited spherical morphology.
• Encapsulation efficiency and mucoadhesion properties were influenced by the type and ratio of mucoadhesive polymers used.
• In vitro dissolution studies indicated a sustained release of furosemide.
• Drug release kinetics best fitted the Higuchi and Korsmeyer-Peppas models, suggesting a non-Fickian diffusion mechanism.

Conclusions:

• Furosemide-loaded mucoadhesive microspheres formulated with sodium alginate and mucoadhesive polymers (HPMC E50 or sodium CMC) show promise for controlled drug delivery.
• The ionic gelation technique and crosslinking with calcium chloride effectively modulated drug release.
• The observed non-Fickian diffusion mechanism provides insights into the drug release behavior from these mucoadhesive systems.