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Schleh, C. ; Semmler-Behnke, M. ; Lipka, J. ; Wenk, A. ; Hirn, S. ; Schäffler, M. ; Schmid, G.* ; Simon, U.* ; Kreyling, W.G.

Size and surface charge of gold nanoparticles determine absorption across intestinal barriers and accumulation in secondary target organs after oral administration.

Nanotox. 6, 36-46 (2012)

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It is of urgent need to identify the exact physico-chemical characteristics, which allow maximum uptake and accumulation in secondary target organs of nanoparticulate drug delivery systems after oral ingestion. We administered radio labelled gold nanoparticles in different sizes (1.4 - 200nm) with negative surface charge and 2.8nm nanoparticles with opposite surface charges by intra-oesophageal instillation into healthy adult female rats. The quantitative amount of the particles in organs, tissues and excrements was measured after 24 hours by gamma-spectroscopy. The highest accumulation in secondary organs was mostly found for 1.4nm particles; the negatively charged particles were accumulated mostly more than positively charged particles. Importantly, 18nm particles show a higher accumulation in brain and heart compared to other sized particles. No general rule accumulation can be made so far. Therefore, specialised drug delivery systems via the oral route have to be individually designed, depending on the respective target organ.

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