Formation of simvastatin nanoparticles from microemulsion

Katy Margulis-Goshen, Shlomo Magdassi*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

80 Scopus citations

Abstract

The present study evaluates a new method to prepare nanoparticles of a poorly water-soluble drug, simvastatin, by evaporation of all solvents from spontaneously formed oil-in-water microemulsions. By this method, microemulsions containing a volatile solvent as an oil phase are converted into nanoparticles in the form of dry non-oily flakes by freeze-drying. The presence of simvastatin in nanoparticles was determined by dispersing the flakes in water and subsequent filtering through a 0.1-μm filter, followed by measuring the simvastatin concentration in the filtrate. It was found that after freeze-drying more than 95% of the drug was present in amorphous particles, smaller than 100 nm. It was found that tablets containing the flakes of simvastatin nanoparticles showed tremendous enhancement in dissolution profile compared with conventional tablets. X-ray diffraction revealed that in the resulting flakes simvastatin nanoparticles were initially amorphous, but a slow crystallization process took place when the product was stored at room temperature. From the Clinical Editor: This paper describes a new method to prepare nanoparticles of a poorly water-soluble drug, simvastatin, by evaporation of all solvents from spontaneously formed oil-in-water microemulsions. Tablets containing the flakes of simvastatin nanoparticles showed tremendous enhancement in dissolution profile compared with conventional tablets.

Original languageAmerican English
Pages (from-to)274-281
Number of pages8
JournalNanomedicine: Nanotechnology, Biology, and Medicine
Volume5
Issue number3
DOIs
StatePublished - Sep 2009

Keywords

  • Evaporation
  • Microemulsion
  • Organic nanoparticles
  • Poorly soluble drug
  • Simvastatin

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