Polyamine Analogues of 3β-[N-(N',N'-Dimethylaminoethane)carbamoyl]cholesterol (DC-Chol) as Agents for Gene Delivery

Gene delivery with cationic liposomes formed from the diamine-lipid DC-Chol and the neutral lipid DOPE has proven successful. New polyamine analogues of DC-Chol have been synthesised, formulated into cationic liposomes with DOPE and biologically tested in vitro and in vivo in mouse lung. Cationic liposomes containing the novel DC-Chol analogue CTAP (shown below) work 100 times more effectively in vivo than DC-Chol containing liposomes (500 times better than DNA alone) and therefore should be suitable for use in human gene therapy approaches towards lung disorders and other clinical conditions.