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    A comparative assessment of nanocomposites vs. amorphous solid dispersions prepared via nanoextrusion for drug dissolution enhancement

    Year: 2017

    Journal: Eur. J. Pharm. Biopharm., Volume 119, OCT, page 68–80

    Authors: Li, Meng; Ioannidis, Nicolas; Gogos, Costas; Bilgili, Ecevit

    Organizations: National Science Foundation Engineering Research Center for Structured Organic Particulate Systems (NSF ERC for SOPS) [EEC-0540855]

    Keywords: Nanocomposites; Amorphous solid dispersion; Nanoextrusion; Spray drying; Nanoparticles; Dissolution

    Nanoextrusion was used to produce extrudates of griseofulvin, a poorly water-soluble drug, with the objective of examining the impact of drug particle size and polymeric matrix type-size of the extrudates on drug dissolution enhancement. Hydroxypropyl cellulose (HPC) and Soluplus (R) were used to stabilize wet-milled drug suspensions and form matrices of the extrudates. The wet-milled suspensions along with additional polymer (HPC/Soluplus (R)) were fed, to a co-rotating twin-screw extruder, which dried the suspensions and formed various extrudates. The extrudates were dry-milled and sieved into samples with two different sizes. A wet-milled suspension was also spray-dried in comparison to nanoextrusion. Due to differences in polymer-drug miscibility, two forms of the drug were prepared: extrudates with nano/micro-crystalline drug particles dispersed in the HPC matrix as a secondary phase (nano/microcomposites) and extrudates with amorphous drug molecularly dispersed within the Soluplus matrix (amorphous solid dispersion, ASD). Under non-supersaturating conditions in the dissolution medium, drug nanocrystals in the HPC-based nanocomposites dissolved faster than the amorphous drug in Soluplus (R)-based ASD. While smaller extrudate particles led to faster drug release for the ASD, such matrix size effect was weaker for the nanocomposites. These findings suggest that nanocrystal-based formulations could outperform ASDs for fast dissolution of low-dose drugs. (C) 2017 Elsevier B.V. All rights reserved.
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