Stabilization of cancer-specific gene carrier via hydrophobic interaction for a clear-cut response to cancer signaling

Chan Woo Kim, Riki Toita, Jeong Hun Kang, Kai Li, Eun Kyung Lee, Guo Xi Zhao, Daiki Funamoto, Takanobu Nobori, Yuta Nakamura, Takeshi Mori, Takuro Niidome, Yoshiki Katayama

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

Here, we developed a new gene carrier, comprising a linear polyethylenimine (LPEI) grafted with a hydro-phobically modified cationic peptide containing a long alkyl chain, for use in cancer-specific gene delivery. The cationic peptide is a substrate of protein kinase Cα (PKCα), which is known to be activated specifically in cancer cells. The hydrophobically modified LPEI-peptide conjugate (LPEI-C10-peptide) could form a polyplex with DNA through electrostatic and hydrophobic interactions between the anionic DNA strands and the cationic peptide substrate. The hydrophobic modification of the peptide did not affect the reactivity of the peptide toward PKCα, while the polyplex showed improved intracellular uptake. Because of the efficient endosomal escape and enhanced stability, the polyplex significantly improved the transgene regulation responding to intracellular PKCα activity.

Original languageEnglish
Pages (from-to)469-476
Number of pages8
JournalJournal of Controlled Release
Volume170
Issue number3
DOIs
Publication statusPublished - Jan 1 2013

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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