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ABSTRACT: Drug delivery, mediated by nanoparticles, relies on nanoparticle stability without drug leakage into the surrounding medium.
Furthermore, nanoparticles have to be taken up by the cells and the payload has to be discharged into the cytoplasm. In order
to test nanoparticle mediated drug delivery we prepared TETD loaded nanoparticles which were stable in phosphate buffered
saline. After mouse fibroblasts were confronted with these nanoparticles cells died at the expected TETD concentration. Since
nanoparticles could be visualized inside the cells by confocal laser scanning microscopy it was assumed that cytoplasmic drug
delivery was successful. However, after measurement of the amount of free TETD in cell culture medium after transfer of the
nanoparticles revealed that TETD was completely discharged from the nanoparticles within several hours. In conclusion, the
observed cytotoxicity of TETD loaded nanoparticles is most likely due to premature release of the TETD into the cell culture
medium acting through the same pathway as TETD applied directly to cells. Therefore it is essential to test for nanoparticle
stability when transferred into another medium.
KeywordsNanoparticle–drug delivery–endocytosis–drug release–TETD
03/2010: pages 65-68;