Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles

J Microencapsul. 2015;32(4):390-400. doi: 10.3109/02652048.2015.1035684. Epub 2015 May 25.

Abstract

Dissolution of poorly water-soluble drug, Artemisinin (ART), was enhanced by encapsulating the drug particles inside pore channels of ordered mesoporous silica, SBA-15, via co-spray drying. The drug release profiles of ART were investigated by using flow-through cell (USP IV) and in vitro dissolution tester (USP II). The co-spray-dried ART/SBA-15 samples demonstrated significantly improved dissolution rates and supersaturation compared to the untreated ART. The low cytotoxicity effect of ART and SBA-15 on Caco-2 cells after 24 h incubation demonstrated the biocompatibility of ART/SBA-15. Finally, the storage stability of the samples was investigated for 6 months under five different storage conditions. Overall, the solid dispersions exhibited excellent physical stability; however, their chemical stability was affected by humidity regardless of storage temperatures. The formulation of solid dispersions of ART/SBA-15 is potentially safe and an effective approach to enhance the solubility of poorly water-soluble ART.

Keywords: Cytotoxicity; chemical stability; drug delivery; excipient; physical stability; supersaturation solubility.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemistry*
  • Anti-Infective Agents / toxicity
  • Artemisinins / chemistry*
  • Artemisinins / toxicity
  • Caco-2 Cells / drug effects
  • Capsules
  • Cell Survival / drug effects
  • Drug Stability
  • Excipients / chemistry*
  • Excipients / toxicity
  • Humans
  • Particle Size
  • Porosity
  • Silicon Dioxide / chemistry*
  • Silicon Dioxide / toxicity
  • Solubility
  • Water / chemistry*

Substances

  • Anti-Infective Agents
  • Artemisinins
  • Capsules
  • Excipients
  • SBA-15
  • Water
  • Silicon Dioxide
  • artemisinin