In the past two decades, different methods have emerged for intervention with gene expression, which can be generally referred to as gene therapy. Oligonucleotides (ONs) and their analogs form the basis of the molecules that can be used to modulate gene expression. Unfortunately, due to their physicochemical properties, these molecules require assistance in their intracellular delivery. Cell-penetrating peptides (CPPs) are one class of nonviral delivery vectors that, because of their remarkable translocation properties, have been intensely utilized for the delivery of ON-based molecules, both in vitro and in vivo. This chapter concentrates on the applications of CPPs that directly form nanoparticles with different ONs and facilitate their intracellular delivery.
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