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Issue 1, 2014
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Stimuli-responsive siRNA carriers for efficient gene silencing in tumors via systemic delivery

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Abstract

Development of efficient carriers for small interfering RNA (siRNA) delivery and validation tools for assessing in vivo RNA interference (RNAi) efficiency is crucial to advance RNAi-based therapeutics to the clinic. Here, acid-degradable ketalized linear polyethylenimine (KL-PEI) designed for efficient, stimuli-responsive, and biocompatible siRNA delivery was used to complex with GFP-silencing siRNA (GFP siRNA) for in vivo RNAi. The in vivo gene silencing efficiency of GFP siRNA/KL-PEI polyplexes was evaluated at mRNA, protein, and histological levels using a mouse bearing a GFP-expressing tumor. Intravenously injected GFP siRNA/KL-PEI polyplexes significantly reduced GFP expression in tumors and whole blood of mice, depending on the dosage of GFP siRNA and the time course. Average GFP mRNA levels in the tumors of siRNA/KL-PEI polyplex-injected mice were also reduced. The described siRNA carriers and RNAi validation methodologies in this study may provide insightful clues for the development of RNAi-based therapeutics and preclinical trials.

Graphical abstract: Stimuli-responsive siRNA carriers for efficient gene silencing in tumors via systemic delivery

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Publication details

The article was received on 03 Aug 2013, accepted on 04 Oct 2013 and first published on 24 Oct 2013


Article type: Communication
DOI: 10.1039/C3BM60187K
Citation: Biomater. Sci., 2014,2, 35-40
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    Stimuli-responsive siRNA carriers for efficient gene silencing in tumors via systemic delivery

    M. S. Shim, S. Chang and Y. J. Kwon, Biomater. Sci., 2014, 2, 35
    DOI: 10.1039/C3BM60187K

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