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BioMed Research International
Volume 2015 (2015), Article ID 406389, 9 pages
http://dx.doi.org/10.1155/2015/406389
Research Article

Low-Molecular-Weight Polyethyleneimine Grafted Polythiophene for Efficient siRNA Delivery

1Nano Medical Engineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan
2Responsive Organic Materials Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan
3Institute of Chemistry, Academia Sinica, 128 Academic Road, Section 2, Nankang, Taipei 11529, Taiwan

Received 4 April 2015; Revised 13 June 2015; Accepted 23 June 2015

Academic Editor: Sanyog Jain

Copyright © 2015 Pan He et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Owing to its hydrophilicity, negative charge, small size, and labile degradation by endogenous nucleases, small interfering RNA (siRNA) delivery must be achieved by a carrier system. In this study, cationic copolymers composed of low-molecular-weight polyethylenimine and polythiophenes were synthesized and evaluated as novel self-tracking siRNA delivery vectors. The concept underlying the design of these copolymers is that hydrophobicity and rigidity of polythiophenes should enhance the transport of siRNA across the cell membrane and endosomal membrane. A gel retardation assay showed that the nanosized complexes formed between the copolymers and siRNA were stable even at a molar ratio of 1 : 2. The high cellular uptake (>80%) and localization of the copolymer vectors inside the cells were easily analyzed by tracking the fluorescence of polythiophene using fluorescent microscopy and cytometry. An in vitro luciferase knockdown (KD) assay in A549-luc cells demonstrated that the siRNA complexes with more hydrophobic copolymers achieved a higher KD efficiency of 52.8% without notable cytotoxicity, indicating protein-specific KD activity rather than solely the cytotoxicity of the materials. Our polythiophene copolymers should serve as novel, efficient, low cell toxicity, and label-free siRNA delivery systems.