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J Control Release. 2012 Dec 28;164(3):387-93. doi: 10.1016/j.jconrel.2012.06.040. Epub 2012 Jul 9.

Cellular delivery of polynucleotides by cationic cyclodextrin polyrotaxanes.

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Department of Drug Delivery, Helmholtz-Institute for Pharmaceutical Research Saarland, Helmholtz-Center for Infection Research (HZI), Saarland University, D-66123 Saarbrücken, Germany.


Cationic polyrotaxanes, obtained by temperature activated threading of cationic cyclodextrin derivatives onto water-soluble cationic polymers (ionenes), form metastable nanometric polyplexes with pDNA and combinations of siRNA with pDNA. Because of their low toxicity, the polyrotaxane polyplexes constitute a very interesting system for the transfection of polynucleotides into mammalian cells. The complexation of Cy3-labeled siRNA within the polyplexes was demonstrated by fluorescence correlation spectroscopy. The uptake of the polyplexes (red) was imaged by confocal fluorescence microscopy using the A549 cell line as a model (blue: nuclei, green: membranes). The results prove the potential of polyrotaxanes for further investigations involving knocking down genes of therapeutic interest.

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