Synthesis and efficient siRNA delivery of polyamine-conjugated cationic nucleoside lipids

Abstract

To advance their use as nonviral gene delivery agents, we have synthesized cationic nucleoside lipids featuring naturally occurring polyamines conjugated at the 5′ position and oleyl groups at the 2′ and 3′ positions of uridine, through chemically stable, but biodegradable, carbamate linkers. The corresponding lipoplexes are efficient and nontoxic vectors for the delivery of siRNA into cells in vitro.