Issue 15, 2015
From the journal:

Chemical Communications

Regulated protonation of polyaspartamide derivatives bearing repeated aminoethylene side chains for efficient intracellular siRNA delivery with minimal cytotoxicity†

Hui Gao,ab   Hiroyasu Takemoto,c   Qixian Chen,b   Mitsuru Naito,b   Hirokuni Uchida,d   Xueying Liu,d   Kanjiro Miyata*d  and  Kazunori Kataoka*bde  

* Corresponding authors

a School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin, China

b Department of Materials Engineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan
E-mail: kataoka@bmw.t.u-tokyo.ac.jp

c Polymer Chemistry Division, Chemical Resources Laboratory, Tokyo Institute of Technology, 4259 Nagatsuta, Midori-ku, Yokohama 226-8503, Japan

d Center for Disease Biology and Integrative Medicine, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan
E-mail: miyata@bmw.t.u-tokyo.ac.jp

e Kawasaki Institute of Industry Promotion, 66-20 Horikawa-cho, Saiwai-ku, Kawasaki 212-0013, Japan

Abstract

The effects of the repeated number (RN) of aminoethylene (AE) units in polyaspartamide side chains were investigated for polyion complex (PIC)-based siRNA delivery. Reduction of the apparent RN from 3 to 2 by thiourea introduction increased a protonatable amine fraction in AE units at endosomal pH, leading to the efficient endosomal escape of siRNA-loaded PICs.

Graphical abstract: Regulated protonation of polyaspartamide derivatives bearing repeated aminoethylene side chains for efficient intracellular siRNA delivery with minimal cytotoxicity

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Article information

DOI
https://doi.org/10.1039/C4CC09859E
Article type
Communication
Submitted
10 Dec 2014
Accepted
09 Jan 2015
First published
09 Jan 2015

Chem. Commun., 2015,51, 3158-3161

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Regulated protonation of polyaspartamide derivatives bearing repeated aminoethylene side chains for efficient intracellular siRNA delivery with minimal cytotoxicity

H. Gao, H. Takemoto, Q. Chen, M. Naito, H. Uchida, X. Liu, K. Miyata and K. Kataoka, Chem. Commun., 2015, 51, 3158 DOI: 10.1039/C4CC09859E

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