Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Aprepitant exhibits poor water solubility, limiting its therapeutic efficacy.
• Developing effective drug delivery systems is crucial for poorly soluble compounds like aprepitant.

Purpose of the Study:

• To improve the physicochemical properties and bioavailability of aprepitant.
• To prepare and characterize solid dispersion (SD) of aprepitant using hydroxypropyl methylcellulose acetate succinate (HPMCAS-LF).

Main Methods:

• Solid dispersion (SD) of aprepitant was prepared using the solvent evaporation method with HPMCAS-LF.
• Characterization involved dissolution testing, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy.
• In vitro permeability was assessed using Caco-2 cell assays.

Main Results:

• The dissolution rate of aprepitant solid dispersion increased fivefold compared to the pure drug.
• Characterization confirmed the presence of amorphous aprepitant within the solid dispersion.
• FTIR analysis indicated intermolecular hydrogen bonding between HPMCAS-LF and aprepitant.
• Caco-2 cell experiments showed enhanced aprepitant permeation without compromising cell integrity (TEER).
• The prepared solid dispersion exhibited excellent stability.

Conclusions:

• Solid dispersion formulation significantly enhances the dissolution rate and permeability of aprepitant.
• HPMCAS-LF is a suitable carrier for creating amorphous solid dispersions of aprepitant.
• This approach offers a promising strategy for improving the oral bioavailability of poorly soluble drugs.