Cholesterol-based cationic lipids for gene delivery: Contribution of molecular structure factors to physico-chemical and biological properties

- A series of cholesterol-based lipid gene carriers were prepared from natural product derived building blocks.
- The cationic headgroups play more important roles than linkages in the physico-chemical properties of the cholesterol-based cationic lipids.
- The cytotoxicity and gene transfection in COS-7 and HeLa cells depend greatly on the types of headgroups.
- The l-lysine headgroup bearing lipids demonstrate very high gene transfection efficacy.
- The correlation between intracellular uptake and gene transfection capacity was studied.