Issue 47, 2017

Functionalized graphene sheets for intracellular controlled release of therapeutic agents

Abstract

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 cells. A pH-sensitive dye was conjugated onto the surfaces of graphene sheets and used as an antenna to obtain specific signals from the acidic cell compartments. It was found that both positively and negatively charged graphene sheets undergo similar acidification processes 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 that from their analogs with a negative surface charge. Therefore, therapeutic efficiency in the first case was much higher than that in the latter. Based on our findings, the intracellular release of drugs from the surfaces 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.

Graphical abstract: Functionalized graphene sheets for intracellular controlled release of therapeutic agents

Supplementary files

Article information

Article type
Paper
Submitted
04 Ndz 2017
Accepted
23 Nhl 2017
First published
03 Huk 2017

Nanoscale, 2017,9, 18931-18939

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, 9, 18931 DOI: 10.1039/C7NR06588D

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements