Non-covalent Nanocomplexes of Folic Acid and Reducible Polyethylenimine for Survivin siRNA Delivery.

Zheng B, Yang S, Wang M, Yang X, Teng L, Xie J, Teng L, Lee RJ
Anticancer Res 35 5433-41 10/01/2015


BACKGROUND/AIM: Efficient delivery of siRNA is critical for its therapeutic applications. This study was aimed at the design, synthesis and evaluation of a novel delivery system based on non-covalent complexes of folic acid (FA) and a reducible polyethylenimine (PEI) derivative, PEI-SS.

MATERIALS AND METHODS: PEI-SS was synthesized by crosslinking low-molecular weight PEI using a reducible crosslinking agent. PEI-SS-siRNA complexes were synthesized and further combined with FA to form FA/PEI-SS-siRNA nanocomplexes. These were then evaluated in two tumor cell lines for survivin siRNA delivery.

RESULTS: FA/PEI-SS-siRNA complexes were taken-up by both HeLa and A549 cells efficiently. This was not affected by the expression level of the folate receptor on the tumor cell surface. Furthermore, FA/PEI-SS-siRNA complexes reduced the level of survivin expression in both cell lines.

CONCLUSION: FA/PEI-SS is a potent siRNA carrier that warrants further evaluation.

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