Polycation liposomes combined with calcium phosphate nanoparticles as a non-viral carrier for siRNA delivery

Low transfection efficiency and instability are the main barriers for siRNA delivery. To overcome these barriers, a core-membrane siRNA delivery system was designed. Calcium phosphate/siRNA nanoparticles were combined with liposomes, and the surface was modified with polyethylenimine-cholesterol (PEI-Chol). The mean particle size of the polycation liposomes/calcium phosphate/siRNA complexes (PLCP) was approximately 260.4 nm and the zeta potential was 0.3 ± 0.2 mV. The buffer capacity and cellular uptake of PLCP were studied. The results indicated that PEI-Chol and CaP can synergistically improve endosomal escape by swelling and disrupting the endosome. Anti-green fluorescent protein (GFP) siRNA was used to evaluate the gene silencing effect in MCF-7 cells that stably express GFP. PLCP could down regulate approximately 70% of GFP expression in 24 h, which is significantly higher than that of Lipofectamine™ 2000. Additionally, the silencing effect lasted for at least 72 h. This delivery system can improve intracellular uptake and enhance gene silencing, with low cytotoxicity.

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