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.
Highlights
In the last few decades, poor aqueous solubility of drugs, resulting in limited bioavailability, has appeared to be one of the major challenges in drug delivery systems [1]
Our findings suggest that the GF release from the Sol-based amorphous solid dispersions (ASDs) was drastically improved owing to the GF wettability enhancement by sodium dodecyl sulfate (SDS) provided that SDS is a minor component with an effective GF recrystallization inhibitor present Sol as the major component in the ternary ASD
While SDS has been commonly used as a solubilizer/carrier typically at 10%–50% in many ternary ASDs, its use as a minor component (
Summary
In the last few decades, poor aqueous solubility of drugs, resulting in limited bioavailability, has appeared to be one of the major challenges in drug delivery systems [1]. Slow and incomplete dissolution of these drugs results in slow absorption in the aqueous environment of the gastrointestinal (GI) tract and eventually low bioavailability. To resolve these challenges, amorphous solid dispersions (ASDs) have been used as an effective platform approach [3,4]. In traditional ASDs, the drug is molecularly dispersed within a hydrophilic/amphiphilic polymeric matrix, resulting in a single-phase amorphous mixture, which inhibits recrystallization of the amorphous drug. As the kinetic solubility of the amorphous drug is higher than that of the crystalline drug, ASDs can enhance the dissolution rate–supersaturation generation significantly [5,6,7]
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