TY - JOUR
T1 - Amphipathic homopolymers for siRNA delivery
T2 - Probing impact of bifunctional polymer composition on transfection
AU - Buerkli, Christian
AU - Lee, Soo Hyeon
AU - Moroz, Elena
AU - Stuparu, Mihaiela C.
AU - Leroux, Jean Christophe
AU - Khan, Anzar
PY - 2014/5/12
Y1 - 2014/5/12
N2 - 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 "proton sponge" effect for siRNA delivery.
AB - 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 "proton sponge" effect for siRNA delivery.
UR - http://www.scopus.com/inward/record.url?scp=84900391215&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84900391215&partnerID=8YFLogxK
U2 - 10.1021/bm5001197
DO - 10.1021/bm5001197
M3 - Article
C2 - 24754338
AN - SCOPUS:84900391215
SN - 1525-7797
VL - 15
SP - 1707
EP - 1715
JO - Biomacromolecules
JF - Biomacromolecules
IS - 5
ER -