Journal
JOURNAL OF CONTROLLED RELEASE
Volume 170, Issue 1, Pages 92-98Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2013.04.013
Keywords
ZNA; Cationic oligonucleotides; Chemically modified siRNA; Lipophilic siRNA; Cholesteryl-siRNA; RNA interference
Funding
- French government (MESR)
- Universite de Strasbourg (Unistra)
- Association Francaise contre les Myopathies (AFM)
- MESR
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Despite its considerable interest in human therapy, in vivo siRNA delivery is still suffering from hurdles of vectorization. We have shown recently efficient gene silencing by non-vectorized cationic siRNA. Here, we describe the synthesis and in vitro evaluation of new amphiphilic cationic siRNA. C12-, (C-12)(2-) and cholesteryl-spermine(x)-siRNA were capable of luciferase knockdown at nanomolar concentrations without vectorization (i.e. one to two orders of magnitude more potent than commercially available cholesteryl siRNA). Moreover, incubation in the presence of serum did not impair their efficiency. Finally, amphiphilic cationic siRNA was pre-loaded on albumin. In A549Luc cells in the presence of serum, these siRNA conjugates were highly effective and had low toxicity. (C) 2013 Published by Elsevier B.V.
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