Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component

Abstract

This study aimed to elucidate the impact of a common anionic surfactant, sodium dodecyl sulfate (SDS), along with hydroxypropyl cellulose (HPC) and Soluplus (Sol) on the release of griseofulvin (GF), a poorly soluble drug, from amorphous solid dispersions (ASDs). Solutions of 2.5% GF and 2.5%–12.5% HPC/Sol with 0.125% SDS/without SDS were prepared in acetone–water and spray-dried. The solid-state characterization of the ASDs suggests that GF–Sol had better miscibility and stronger interactions than GF–HPC and formed XRPD-amorphous GF, whereas HPC-based ASDs, especially the ones with a lower HPC loading, had crystalline GF. The dissolution tests show that without SDS, ASDs provided limited GF supersaturation (max. 250%) due to poor wettability of Sol-based ASDs and extensive GF recrystallization in HPC-based ASDs (max. 50%). Sol-based ASDs with SDS exhibited a dramatic increase in supersaturation (max. 570%), especially at a higher Sol loading, whereas HPC-based ASDs with SDS did not. SDS did not interfere with Sol’s ability to inhibit GF recrystallization, as confirmed by the precipitation from the supersaturated state and PLM imaging. The favorable use of SDS in a ternary ASD was attributed to both the wettability enhancement and its inability to promote GF recrystallization when used as a minor component along with Sol.

Dry Dosage Forms of Add-Value Bioactive Phenolic Compounds by Supercritical CO2-Assisted Spray-Drying

“…Figure S3 (Supplementary Materials) shows that XRPD diffractograms revealed that both non-processed HPC and processed HPC exhibited two peaks at about 8° and 20°, indicating that this polymer has an amorphous domain. This aligns with data by Rahman et al [ 37 ] that confirmed the same peaks for non-processed HPC. Differing HPC concentrations depicted the same peaks, although their intensity was shown to be slightly lower for the SASD HPC.…”

“…In addition, the literature has also reported a few small crystalline peaks between 29–47° [ 38 ]. Rahman et al [ 37 ] uncovered a small endothermic peak around 190–200 °C for the DSC thermogram of raw HPC. This probably results from the fusion of the small crystalline fraction of largely amorphous HPC or a liquid crystal isotropic transition [ 39 , 40 ].…”

Analytical and Computational Methods for the Determination of Drug-Polymer Solubility and Miscibility

“…Greenhalgh et al and Hancock et al have suggested that the system can be considered miscible if the difference between the solubility parameter value of components is less than 7 MPa 1/2 , while the difference greater than 10 MPa 1/2 should be considered as a sign of immiscibility. , Schilling et al have used these criteria to conclude miscibility between diltiazem hydrochloride and citric acid . Sathigari et al and Prasad et al have used these criteria to demonstrate the miscibility of eudragit EPO with efavirenz and indomethacin, respectively. , Apart from this, numerous reports have discussed the difference in the solubility parameter as an indicator of drug-polymer miscibility. − …”

Safety and Pharmaceutical Evaluation of a Novel Natural Polymer, Ocicum, as Solubility and Dissolution Enhancer in Solid Dispersion

“…These are among the simplest dosage forms, and may contain the drug and polymer in a binary solid-dispersion system while additionally containing surfactant in a tertiary system. Solid dispersions can be fabricated by using different methods, such as solvent evaporation [ 6 ], melting method [ 10 ], spray drying [ 11 ], hot melt extrusion, supercritical fluid technology [ 12 ] and electrostatic spinning [ 13 ]. However, one of the most promising and cheap methods is solvent evaporation, which involves digestion of the drug and carrier in single or multiple solvents to make a clear solution, followed by solvent evaporation [ 5 , 14 ].…”