Development of uniform fenofibrate-loaded biodegradable microparticle by membrane emulsification

Area of Science:

• Biomaterials Science
• Ophthalmology
• Drug Delivery

Background:

• Fenofibrate shows therapeutic potential for diabetic retinopathy.
• Rapid clearance of fenofibrate after intravitreal injection limits its efficacy.

Purpose of the Study:

• To develop fenofibrate-loaded PLGA microparticles (Feno-MP) for sustained intravitreal drug delivery.
• Achieve high drug loading and in vitro release for up to 6 months.

Main Methods:

• Formulation optimization using orthogonal array experimental design.
• Fabrication of Feno-MP via homogenization and direct membrane emulsification.
• Characterization of particle size, drug loading, and in vitro release kinetics.

Main Results:

• Both methods yielded Feno-MP with high drug loading and sustained release (>140 days).
• Membrane emulsification produced uniform-sized Feno-MP, unlike the polydisperse particles from homogenization.
• Larger Feno-MP (8-16 µm) exhibited higher drug loading and more sustained release with reduced burst release compared to smaller particles (1.5 µm).

Conclusions:

• Developed Feno-MP with high drug loading and sustained release profile for intravitreal injection.
• Particle size significantly impacts drug loading and release kinetics.
• Membrane emulsification offers a method for producing uniform Feno-MP, enhancing batch-to-batch reproducibility.