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Functionalized Graphene Sheets for Intracellular Controlled Release of Therapeutic Agents


Since therapeutic agents target specific compartments inside the cells, their efficiency depends on their intracellular release from drug delivery systems (DDS). However, control over the intracellular release of therapeutic agents is a challenging issue and can only be achieved by governing their interactions with the DDS. In this work, polyglycerol amine- and polyglycerol sulfate-functionalized graphene sheets as positively and negatively charged 2D nanomaterials with 150 nm lateral size were used to deliver and control the release of doxorubicin (DOX) inside the cells. A pH-sensitive dye was conjugated onto the surfaces of graphene sheets and used as an antenna to obtain specific signals in the acidic cell compartments. It was found that both positively and negatively charged graphene sheets undergo the similar acidification process after cellular uptake. Nevertheless, the intracellular drug release of these DOX-loaded nanomaterials was distinctly different. As an overall effect of the π-π stacking and electrostatic interactions, the release of DOX from the positively charged graphene sheets was much faster than their analogs with the negative surface charge. Therefore, therapeutic efficiency in the first case was much higher than in the latter. Based on our findings, intracellular release of drugs from the surface of graphene sheets can be finely tuned by manipulating their functionalities, which is of great importance in the designing of the future graphene-based nanomedicines.

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Publication details

The article was received on 04 Sep 2017, accepted on 23 Oct 2017 and first published on 03 Nov 2017

Article type: Paper
DOI: 10.1039/C7NR06588D
Citation: Nanoscale, 2017, Accepted Manuscript
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    Functionalized Graphene Sheets for Intracellular Controlled Release of Therapeutic Agents

    Z. Tu, V. Wycisk, C. Cheng, W. Chen, M. Adeli and R. Haag, Nanoscale, 2017, Accepted Manuscript , DOI: 10.1039/C7NR06588D

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