(790j) Spray Drying of Griseofulvin Nanosuspensions and Solutions for Preparation of Nanocomposites and Amorphous Solid Dispersions: Comparative Assessment of Drug Release

BCS class II drugs are compounds that are poorly water-soluble and exhibit high permeability. In order to increase the dissolution rate and bioavailability of these compounds, two specific processes can be used: amorphous solid dispersions (ASD) and nanocomposites. ASD’s disrupt the drug crystal lattice which causes an increase in the saturation solubility, whereas nanocomposites exhibit very large surface areas; both of which cause a faster dissolution. The goal of this project is to compare the release of the active pharmaceutical ingredient Griseofulvin (GF) from nanocomposites and that from ASD’s, both having identical formulations.

GF nanocomposites were prepared by wet media milling (nanomilling) an aqueous GF suspension followed by spray drying. Two different polymers, hydroxypropyl cellulose (HPC) and Soluplus, with an anionic surfactant, sodium dodecyl sulfate (SDS), were used for the stabilization of drug nanoparticles. ASD’s were formulated by spray drying the respective drug-polymer in acetone-DI water. The suspensions were characterized via laser diffraction, while the spray-dried powders were characterized via laser diffraction, X-ray diffraction (XRD), and dissolution testing. XRD diffractograms confirmed that for both polymers, spray drying of the aqueous nanosuspension led to nanocomposites, whereas that of the drug solution led to ASD. At supersaturating conditions, drug dissolution from ASD was faster than that from the nanocomposites.