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Issue 43, 2016
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A facile modular approach toward multifunctional supramolecular polyplexes for targeting gene delivery

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Abstract

Extensive efforts and numerous methodologies have been explored to develop safe and efficient gene carriers that are capable of overcoming multiple extra- and intracellular barriers during the transfection process. However, it is a great challenge to fabricate a gene carrier system containing multiple functional components. In this work, we propose a facile modular approach to design targeted multifunctional gene delivery systems, which are based on building blocks with pre-defined functions to tackle specific barriers. These building blocks can be rationally combined and self-assemble into an integrated gene delivery system via host–guest interactions. As a proof of concept, three adamantyl-terminated targeting guest modules, adamantyl terminated RGD peptide (Ad-RGD), folate and lactobionic acid terminated PEGs (FA-PEG-Ad and LA-PEG-Ad), were synthesized, characterized, and utilized for post-functionalizing of adamantyl decorated cationic PEI based supramolecular polyplexes (PEI-Ad4/PCD/DNA) through the free CD units of the poly(β-cyclodextran) (PCD) host module. These multifunctional targeting supramolecular polyplexes exhibited enhanced cellular uptake and excellent transfection activity in receptor-positive cells. By modulating the functional components of the supramolecular platform, we can customize the gene carriers for further research on different tissues or cells in vitro or in vivo.

Graphical abstract: A facile modular approach toward multifunctional supramolecular polyplexes for targeting gene delivery

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Publication details

The article was received on 06 Jul 2016, accepted on 04 Oct 2016 and first published on 04 Oct 2016


Article type: Paper
DOI: 10.1039/C6TB01671E
Citation: J. Mater. Chem. B, 2016,4, 7022-7030
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    A facile modular approach toward multifunctional supramolecular polyplexes for targeting gene delivery

    J. Liu, W. E. Hennink, M. J. van Steenbergen, R. Zhuo and X. Jiang, J. Mater. Chem. B, 2016, 4, 7022
    DOI: 10.1039/C6TB01671E

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