Intracellular delivery of siRNA by cell-penetrating peptides modified with cationic oligopeptides

Tsutomu Ishihara, Maoko Goto, Kanae Kodera, Hideko Kanazawa, Yasuko Murakami, Yutaka Mizushima, Megumu Higaki

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)


To achieve the effective intracellular delivery of siRNA and silence specific genes, various types of conjugates between cell-penetrating peptides (CPPs; Transportan, Penetratin, Tat) and cationic peptides were developed. Uptake, intracellular localization, cytotoxicity, and biological activity of siRNA were significantly dependent on the kind of CPP used and the length of the cationic peptides in the conjugate. Transportan-based conjugates yielded both high internalization of siRNA and strong gene silencing activity, while Penetratin- and Tat-based conjugates did not. These different properties of CPPs emphasize the importance of careful peptide selection and design when attempting the application of CPP technology.

Original languageEnglish
Pages (from-to)153-159
Number of pages7
JournalDrug delivery
Issue number3
Publication statusPublished - 2009


  • Cationic peptide
  • Cell-penetrating peptide
  • Endocytosis
  • Intracellular delivery
  • SiRNA

ASJC Scopus subject areas

  • Pharmaceutical Science


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