Cell-penetrating cationic siRNA and lipophilic derivatives efficient at nanomolar concentrations in the presence of serum and albumin
| Autor: | Jean-Paul Behr, Marc Nothisen, Jean-Serge Remy, Mitsuharu Kotera, Jérémy Bagilet, Phanélie Perche |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Serum
Gene knockdown Chemistry Cell Oligonucleotides Albumin Cationic polymerization Pharmaceutical Science Lipids In vitro medicine.anatomical_structure Biochemistry Luciferases Firefly In vivo Albumins Cell Line Tumor medicine Humans Gene silencing Spermine Luciferase Gene Silencing RNA Small Interfering |
| Zdroj: | Journal of Controlled Release. 170:92-98 |
| ISSN: | 0168-3659 |
| DOI: | 10.1016/j.jconrel.2013.04.013 |
| Popis: | 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. C 12 -, (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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect