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

Meng Li, Nicolas Ioannidis, Costas Gogos, Ecevit Bilgili

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

Abstract

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® were used to stabilize wet-milled drug suspensions and form matrices of the extrudates. The wet-milled suspensions along with additional polymer (HPC/Soluplus®) 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®-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.

Original languageEnglish (US)
Pages (from-to)68-80
Number of pages13
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume119
DOIs
StatePublished - Oct 2017

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Pharmaceutical Science

Keywords

  • Amorphous solid dispersion
  • Dissolution
  • Nanocomposites
  • Nanoextrusion
  • Nanoparticles
  • Spray drying

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