We report here that a synthesized multivalent cationic lipopeptide can be used for the delivery and release of gene assembled into lipopeptide vesicles. It is found experimentally that the synthesized lipopeptide is safe for gene therapy because of its biocompatibility and the innocuity of the hydrolysis products, such as lipids and amino acids. The experimental results also show that the assembled DNA/lipopeptide complex has high transfection efficiency in HeLa cells compared to that of the selected commercial reagent, which represents a novel vector for the delivery of therapeutic DNA.