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 journalArticleScientificpeer-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 nano-sized material with the physiological environment during the delivery process is required. In the present study, the behaviour of thermally oxidized porous silicon (TOPSi) 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-? 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-? 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
    Publication statusPublished - 2011
    Publication typeA1 Journal article-refereed


    • 317 Pharmacy
    • epithelial cell
    • macrophage
    • cytotoxicity
    • 116 Chemical sciences
    • nanoparticle
    • silicon
    • degradation


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