Amphipathic Homopolymers for siRNA Delivery: Probing Impact of Bifunctional Polymer Composition on Transfection

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• 作者：Christian Buerkli ; Soo Hyeon Lee ; Elena Moroz ; Mihaiela C. Stuparu ; Jean-Christophe Leroux ; Anzar Khan
• 刊名：Biomacromolecules
• 出版年：2014
• 出版时间：May 12, 2014
• 年：2014
• 卷：15
• 期：5
• 页码：1707-1715
• 全文大小：499K
• 年卷期：v.15,no.5(May 12, 2014)
• ISSN：1526-4602

文摘

In this study, we systematically explore the influence of the lipophilic group on the siRNA transfection properties of the polycationic-based delivery vectors. For this, a novel and modular synthetic strategy was developed for the preparation of polymers carrying a cationic site and a lipophilic group at each polymer repeat unit. These bifunctional polymers could form a complex with siRNA and deliver it to human colon carcinoma cells (HT-29-luc). In general, transfection capability increased with an increase in the chain length of the lipophilic moiety. The best transfection agent, a polymer containing ammonium groups and pentyl side chains, exhibited lower toxicity and higher transfection efficiency than branched and linear polyethylenimines (PEI). Moreover, as opposed to PEI, the transfection efficiency of polymer/siRNA complexes remained unchanged in the presence of bafilomycin A1, a proton pump inhibitor, suggesting that the present system did not rely on the 鈥減roton sponge鈥?effect for siRNA delivery.