Novel lipoidal amine-based nanocarrier formulations for siRNA delivery.

Lack of safe and efficient delivery of siRNA remains the greatest hurdle for the therapeutic application of siRNA. This article reports synthesis and evaluation of novel lipoidal amine-based nanocarrier (LANC) formulations for siRNA delivery. Physicochemical properties were analyzed for LANC formulations. siRNA delivery efficiency of LANC-siRNA complexes was determined using a luciferase reporter gene assay. Cytotoxicity of the LANC-siRNA complexes was measured by the MTS assay. Finally, cellular uptake and cytoplasmic release of siRNA were analyzed using flow cytometry. The LANC formulation facilitated siRNA uptake and release into the cytoplasm, mediating significant luciferase knockdown (70% inhibition).