Interlock Protective System from Hyperbranched Polyethyleneimine and Choline Phosphate Liposome for Targeted In Vivo Gene Delivery

Abstract Both hyperbranched polyethyleneimine (hPEI) and cationic lipids exhibit excellent gene transfection efficiency, while their high toxicity, easily to be cleared in the blood, and have no targeting effect, which severely limits their application in in vivo gene delivery. In view of the above problems, the synergistic effects between hPEI and choline phosphate lipid (CP‐lip) are used to develop an interlock protective system to deliver genes in vivo which combines stability, transfection efficiency, and biosafety. In this work, DNA, hPEI, and CP‐lips are combined and interacted strongly to form a targeted liposome (tCP‐lipo/(PEI/DNA)). This interlock protective system could deliver genes to tumor sites after circulate in the blood with safety, then the loaded genes are transfected to kill cancer cells. The interlock protection system constructed by CP‐lips and hPEI provides an efficient and safe platform for targeted gene delivery in vivo.