Ginsenoside as a new stabilizer enhances the transfection efficiency and biocompatibility of cationic liposome.

Nucleic acid drugs have emerged as important therapeutics, but their clinical application has been greatly limited by their large molecular weight, high polarity, negative charge and short half-life. Cationic liposomes (CLs) have gained wide attention as non-viral vectors for nucleic acids delivery. However, the absolute transfection efficiency of CLs is still to be enhanced with cytotoxicity to be decreased simultaneously. Ginsenosides, separated from natural plants, possess the similar steroid structure to cholesterol and might be the alternative to cholesterol for acting as membrane stabilizer of CLs. Herein, seven kinds of ginsenosides-based compounds were utilized to prepare CLs (GCLs) and their efficacy in siRNA delivery were investigated. The particle sizes of the GCLs were 90~300 nm and the SiRNAs delivery efficiency are 23.6%-78.4%. Rg5-based CLs (Rg5-CLs) exhibited the highest transfection efficiency of 81% and the lowest toxicity, with 82% cells viability was obtained evnen at the high concentration. Ginsenosides are shown as the promising biomaterials as the membrane stabilzer of CLs. Rg5-CLs are demonstrated as the efficient non-viral vectors with high transfection efficiency and good biocompatibility of gene delivery, possessing great potential for gene therapy