Drug permeation across intestinal epithelial cells using porous silicon nanoparticles

Luis M. Bimbo, Ermei Mäkilä, Timo Laaksonen, Vesa-Pekka Lehto, Jarno Salonen, Jouni Hirvonen, Hélder A. Santos

Research output: Contribution to journalArticlepeer-review

146 Citations (Scopus)


Mesoporous silicon particles hold great potential in improving the solubility of otherwise poorly soluble drugs. To effectively translate this feature into the clinic, especially via oral or parenteral administration, a thorough understanding of the interactions of the micro- and nanosized material with the physiological environment during the delivery process is required. In the present study, the behaviour of thermally oxidized porous silicon particles of different sizes interacting with Caco-2 cells (both non-differentiated and polarized monolayers) was investigated in order to establish their fate in a model of intestinal epithelial cell barrier. Particle interactions and TNF-α were measured in RAW 264.7 macrophages, while cell viabilities, reactive oxygen species and nitric oxide levels, together with transmission electron microscope images of the polarized monolayers, were assessed with both the Caco-2 cells and RAW 264.7 macrophages. The results showed a concentration and size dependent influence on cell viability and ROS-, NO- and TNF-α levels. There was no evidence of the porous nanoparticles crossing the Caco-2 cell monolayers, yet increased permeation of the loaded poorly soluble drug, griseofulvin, was shown.

Original languageEnglish
Pages (from-to)2625-2633
Number of pages9
Issue number10
Early online date30 Dec 2010
Publication statusPublished - 30 Apr 2011
Externally publishedYes


  • animals
  • Caco-2 cells
  • cell death
  • cell membrane permeability
  • cell survival
  • epithelial cells
  • griseofulvin
  • humans
  • inflammation
  • intestines
  • intracellular space
  • macrophages
  • mice
  • nanoparticles
  • nitric oxide
  • oxidation-reduction
  • porosity
  • reactive oxygen species
  • silicon
  • solubility
  • temperature
  • tumor necrosis factor-alpha


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