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Issue 28, 2017
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Head group configuration increases the biocompatibility of cationic lipids for nucleic acid delivery

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Abstract

Intracellular delivery of genetic material is a potentially powerful therapeutic approach for the treatment of genetic diseases. However, the scarcity of biocompatible delivery systems is a tremendous barrier for the application of nucleic acid therapy in the clinic. Herein, we successfully created biocompatible nucleic acid delivery systems based on cationic lipids consisting of alternatively linked ornithine residues in the head group (denoted DoGo lipids). Transfection of the pcDNA3-eGFP plasmid into cells using DoGo lipids resulted in significant transfection efficiency without showing any apparent cytotoxicity. Meanwhile, DoGo lipids efficiently delivered siRNA to cancer cell lines and induced profound RNAi activity at a siRNA concentration as low as 5 nM. DoGo lipid driven delivery of a siRNA against polo-like kinase 1 (Plk1) in cancer cells induced significant morphological changes in the cell and the nucleus due to cell cycle arrest and inhibition of cell proliferation, a phenotype resulting from the decreased Plk1 protein level. Our findings demonstrate that DoGo lipids have great potential in clinical application for gene based therapy.

Graphical abstract: Head group configuration increases the biocompatibility of cationic lipids for nucleic acid delivery

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Publication details

The article was received on 30 Jan 2017, accepted on 21 Jun 2017 and first published on 22 Jun 2017


Article type: Paper
DOI: 10.1039/C7TB00317J
Citation: J. Mater. Chem. B, 2017,5, 5597-5607
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    Head group configuration increases the biocompatibility of cationic lipids for nucleic acid delivery

    G. Gerile, T. Ganbold, Y. Li and H. Baigude, J. Mater. Chem. B, 2017, 5, 5597
    DOI: 10.1039/C7TB00317J

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