Eudragit(®) microparticles for the release of budesonide: a comparative study

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Budesonide is a potent anti-inflammatory corticosteroid used to treat inflammatory bowel diseases.
• Developing effective drug delivery systems is crucial for targeted budesonide delivery and improved therapeutic outcomes.

Purpose of the Study:

• To compare the characteristics and in vitro performance of budesonide-loaded microparticles formulated with Eudragit®RS or a Eudragit®RS/Eudragit®RL blend.
• To evaluate the influence of preparation techniques (solvent evaporation vs. spray-drying) on microparticle properties and drug release.

Main Methods:

• Microparticles were prepared using solvent evaporation and spray-drying techniques with Eudragit®RS or Eudragit®RS/Eudragit®RL (70:30 w/w).
• Loading efficiency was determined, and thermal analyses were conducted to assess drug-polymer interactions and structural stability.
• In vitro drug release studies were performed in simulated gastric and intestinal fluids.

Main Results:

• Spray-dried microparticles exhibited slightly higher budesonide loading efficiency (approx. 78%) compared to solvent-evaporated ones (approx. 72%).
• Eudragit®RS/Eudragit®RL microparticles showed a significantly higher drug release (approx. 6-fold) in simulated gastric fluid compared to Eudragit®RS microparticles.
• In simulated intestinal fluid, drug release was limited (4-30%) for both formulations.
• Eudragit®RS microparticles provided better protection against gastric acidity.

Conclusions:

• Eudragit®RS microparticles demonstrate enhanced stability in simulated gastric fluid.
• The findings suggest Eudragit®RS microparticles are a promising candidate for colon-specific controlled delivery of budesonide.