Abstract In this work, we have successfully prepared a series of new sterol-based cationic lipids (1–4) via an efficient 'Click'chemistry approach. The pDNA binding affinity of these lipids was examined by EB displacement and agarose-gel retardant assay. The average particle sizes and surface charges of the sterol-based cationic lipids/pDNA lipoplexes were analyzed by dynamic laser light scattering instrument (DLS), and the morphologies of the ...