Acidic pH-Responsive siRNA Conjugate for Reversible Carrier Stability and Accelerated Endosomal Escape with Reduced IFNα-Associated Immune Response

An siRNA conjugate is based on an acid‐labile maleic acid amide linkage for programmed transfer of siRNA from the endosome to the cytosol and siRNA release in the cell interior. The procedure relies on reversible stability in response to endosomal acidic pH value. The complexed polyionic conjugate a...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2013-06, Vol.52 (24), p.6218-6221
Main Authors: Takemoto, Hiroyasu, Miyata, Kanjiro, Hattori, Shota, Ishii, Takehiko, Suma, Tomoya, Uchida, Satoshi, Nishiyama, Nobuhiro, Kataoka, Kazunori
Format: Article
Language:English
Subjects:
Acids - metabolism
conjugation
drug delivery
drug design
Endosomes - metabolism
Hydrogen-Ion Concentration
Interferon-alpha - metabolism
polymers
RNA, Small Interfering - metabolism
siRNA
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Summary:An siRNA conjugate is based on an acid‐labile maleic acid amide linkage for programmed transfer of siRNA from the endosome to the cytosol and siRNA release in the cell interior. The procedure relies on reversible stability in response to endosomal acidic pH value. The complexed polyionic conjugate achieved gene silencing in cultured cancerous cells with negligible side effects.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201300178