Conjugate for efficient delivery of short interfering RNA (siRNA) into mammalian cells

Abstract

The efficient delivery of short interfering RNAs (siRNAs) into cells provides a powerful approach to study cellular functions. SiRNAs were coupled to the membrane permeant peptides (MPPs) penetratin and transportan to improve their uptake by cells. Thiol‐containing siRNAs corresponding to luciferase, or green fluorescent protein ( GFP ) transgenes, were synthesized and conjugated to penetratin or transportan via a disulfide bond that is labile in the reducing environment of the cytoplasm. These MPP‐siRNAs efficiently reduced transient and stable expression of reporter transgenes in several mammalian cell types in a high proportion of cells, and demonstrated equivalent or better delivery characteristics than cationic liposomes with fewer manipulations.