Electrosprayed microparticles for intestinal delivery of prednisolone

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Polymer Science

Background:

• Eudragit L100-55 is a pH-responsive polymer suitable for targeted drug delivery.
• Prednisolone is an active pharmaceutical ingredient used for inflammatory conditions.
• Site-specific drug release is crucial for treating gastrointestinal diseases like inflammatory bowel disease and colon cancer.

Purpose of the Study:

• To prepare and characterize Eudragit L100-55 microparticles containing prednisolone.
• To evaluate the drug release profile of the microparticles under different pH conditions.
• To assess the potential of the developed system for site-specific delivery of prednisolone.

Main Methods:

• Single and coaxial electrospraying techniques were employed for microparticle preparation.
• Five different formulations with varying polymer:drug ratios were developed.
• X-ray diffraction analysis confirmed the amorphous state of prednisolone.
• Dissolution studies were conducted to assess drug release kinetics.

Main Results:

• Toroidal-shaped microparticles with narrow size distribution were successfully prepared.
• Prednisolone was found to be in an amorphous physical state within the microparticles.
• The Eudragit L100-55 microparticles demonstrated pH-dependent drug release.
• Minimal prednisolone release occurred in acidic conditions (pH < 6.8), followed by rapid release at pH 6.8.

Conclusions:

• Electrospraying is an effective method for producing Eudragit L100-55 microparticles containing prednisolone.
• The pH-responsive nature of Eudragit L100-55 enables site-specific drug release, minimizing gastric irritation.
• This formulation holds promise for targeted delivery of prednisolone for inflammatory bowel disease and colon cancer treatment.