Issue 39, 2016

Block ionomer complexes consisting of siRNA and aRAFT-synthesized hydrophilic-block-cationic copolymers II: the influence of cationic block charge density on gene suppression

Abstract

Block ionomer complex (BIC)–siRNA interactions and effectiveness in cell transfection are reported. Aqueous RAFT polymerization was used to prepare a series of hydrophilic-block-cationic copolymers in which the cationic block statistically incorporates increasing amounts of neutral, hydrophilic monomer such that the number of cationic groups remains unchanged but the cationic charge density is diluted along the polymer backbone. Reduced charge density decreases the electrostatic binding strength between copolymers and siRNA with the goal of improving siRNA release after targeted cellular delivery. However, lower binding strength resulted in decreased transfection and RNA interference pathway activation, leading to reduced gene knockdown. Enzymatic siRNA degradation studies with BICs indicated lowered binding strength increases susceptibility to RNases, which is the likely cause for poor gene knockdown.

Graphical abstract: Block ionomer complexes consisting of siRNA and aRAFT-synthesized hydrophilic-block-cationic copolymers II: the influence of cationic block charge density on gene suppression

Supplementary files

Article information

Article type
Paper
Submitted
16 Jun 2016
Accepted
08 Aug 2016
First published
08 Aug 2016

Polym. Chem., 2016,7, 6044-6054

Block ionomer complexes consisting of siRNA and aRAFT-synthesized hydrophilic-block-cationic copolymers II: the influence of cationic block charge density on gene suppression

K. H. Parsons, A. C. Holley, G. A. Munn, A. S. Flynt and C. L. McCormick, Polym. Chem., 2016, 7, 6044 DOI: 10.1039/C6PY01048B

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