Abstract

In this study, we describe the development of a new siRNA delivery method for enhanced gene silencing, which is based on HER2 RNA aptamer‐ and cell penetrating peptide (CPP)‐mediated intracellular delivery of multimeric antisense strands of siRNAs. By making use of HER2 RNA aptamer or peptide nucleic acid‐linked CPP as delivery moiety for multimeric antisense strands of siRNAs, the multimeric siRNAs were observed to show significant gene silencing effects even without any delivery vehicles, in comparison with the conventional duplexed monomeric siRNAs mixed with lipofectamine. Our observations suggest that the introduction of RNA aptamer or CPP to multimeric siRNA as delivery moiety of siRNA delivery system can allow efficient target gene suppression with slow and steady but persistent intracellular uptake capacity.

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