Electrospinner: Preparation of fenofibrate solid dispersion by electrostatic spray deposition and improvement of oral absorption by transient post-heating of the preparation

Objective and Methods

Objective: To improve the bioavailability of the poorly soluble drug fenofibrate.

Methods: Core-shell solid dispersions were prepared using coaxial electrostatic spray technology, with polymethacrylic acid-methyl methacrylate (Eudragit L-100) as the shell material and polyvinylpyrrolidone K12-17 (PVP) as the core phase dispersant.

Results

Electrostatic spray preparation: In the electrostatic spray preparation, 58% of FEN was still in the crystalline state, but the dissolution behavior was significantly improved by reducing the particle size, reducing the crystallinity and improving the dispersion efficiency.

Post-heating treatment: The preparation was post-heated at 100°C for 30 seconds to convert the remaining crystals into an amorphous state, further improving the dissolution behavior and oral bioavailability.

Oral bioavailability: The bioavailability of the heated preparation was the highest, followed by the original preparation, and the lowest was crystalline FEN.

Analysis

Advantages of the core-shell structure: The core-shell structure can protect the core drug from the external environment and improve stability and bioavailability.

Electrostatic spraying technology: This technology is able to work under room temperature and pressure conditions, is suitable for nano- and amorphization, and helps improve the dissolution of poorly soluble drugs.

Effect of post-heating: The simple post-heating procedure significantly improved the performance of the formulation, indicating that post-heating can be used as a powerful step in the formulation production process.

Physical stability of the formulation: The physical stability of the formulation was improved by reducing the crystallinity, which is particularly important for amorphous formulations.

Glass-forming ability of the drug: FEN has a high glass-forming ability, making the post-heating method applicable, but this method may also be applicable to drugs with lower glass-forming ability.

Conclusion

The study successfully prepared the core-shell solid dispersion of fenofibrate using coaxial electrostatic spraying technology, and further improved the performance of the formulation by post-heating treatment. This method not only improves the bioavailability of poorly soluble drugs, but also provides a simple and effective post-treatment step for formulation production. This study provides a valuable reference for improving the dissolution and bioavailability of poorly soluble drugs.

Electrospinning Nanofibers Article Source:

10.1016/jijpharm.2013.04.006