Formulation optimization of double emulsification method for preparation of enzyme-loaded Eudragit S100 microspheres

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Serratiopeptidase is an acid-labile enzyme requiring protection for oral delivery.
• Developing sustained-release microparticulate systems is crucial for improving oral bioavailability of such enzymes.

Purpose of the Study:

• To develop an oral sustained release microparticulate system for Serratiopeptidase.
• To optimize Eudragit S100 microspheres using a 3(2) full factorial design.
• To investigate the impact of formulation variables on microsphere characteristics and enzyme activity.

Main Methods:

• Modified double emulsion solvent evaporation technique for microsphere preparation.
• 3(2) full factorial design to study external aqueous phase volume and Tween 80 concentration.
• Scanning electron microscopy (SEM) for particle morphology analysis.
• In vitro proteolytic activity assay to confirm enzyme integrity and release kinetics.

Main Results:

• External aqueous phase volume significantly affected entrapment efficiency; Tween 80 concentration significantly impacted microsphere size.
• Optimized microspheres exhibited smooth spherical morphology with high drug encapsulation (81.32 ± 3.97%).
• Controlled enzyme release observed: minimal release at pH 1.2 and sustained release in phosphate buffer, following Higuchi kinetics (R(2) = 0.987).

Conclusions:

• The study successfully developed an optimized Eudragit S100 microparticulate system for oral sustained release of Serratiopeptidase.
• The formulation optimization using factorial design proved economical and efficient.
• The developed system ensures enzyme stability and controlled release, enhancing therapeutic potential.