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Short nucleic acids targeting biologically important RNAs and plasmids have been shown to be promising future therapeutics; however, their hydrophilic nature greatly limits their utility in clinics and therefore efficient delivery vectors are greatly needed. Cell-penetrating peptides (CPPs) are relatively short amphipathic and/or cationic peptides that are able to transport various biologically active molecules inside mammalian cells, both in vitro and in vivo, in a seemingly non-toxic fashion. Although CPPs have proved to be appealing drug delivery vehicles, their major limitation in nucleic acid delivery is that most of the internalized peptide-cargo is entrapped in endosomal compartments following endocytosis and the bioavailability is therefore severely reduced. Several groups are working towards overcoming this obstacle and this review highlights the evidence that by introducing chemical modification in CPPs, the bioavailability of delivered nucleic acids increases significantly.

Original publication

DOI

10.1517/17425240903213688

Type

Journal article

Journal

Expert Opin Drug Deliv

Publication Date

11/2009

Volume

6

Pages

1195 - 1205

Keywords

Animals, Antisense Elements (Genetics), Biological Availability, Drug Carriers, Drug Delivery Systems, Endocytosis, Gene Transfer Techniques, Humans, Peptides, Surface-Active Agents