PMID- 26539490 OWN - NLM STAT- MEDLINE DCOM- 20160818 LR - 20240325 IS - 2314-6141 (Electronic) IS - 2314-6133 (Print) VI - 2015 DP - 2015 TI - Low-Molecular-Weight Polyethyleneimine Grafted Polythiophene for Efficient siRNA Delivery. PG - 406389 LID - 10.1155/2015/406389 [doi] LID - 406389 AB - 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. FAU - He, Pan AU - He P AD - Nano Medical Engineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. FAU - Hagiwara, Kyoji AU - Hagiwara K AD - Nano Medical Engineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. FAU - Chong, Hui AU - Chong H AD - Responsive Organic Materials Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. FAU - Yu, Hsiao-hua AU - Yu HH AD - Responsive Organic Materials Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan ; Institute of Chemistry, Academia Sinica, 128 Academic Road, Section 2, Nankang, Taipei 11529, Taiwan. FAU - Ito, Yoshihiro AU - Ito Y AD - Nano Medical Engineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20151011 PL - United States TA - Biomed Res Int JT - BioMed research international JID - 101600173 RN - 0 (Cations) RN - 0 (Polymers) RN - 0 (RNA, Small Interfering) RN - 0 (Thiophenes) RN - 25233-34-5 (polythiophene) RN - 9002-98-6 (Polyethyleneimine) SB - IM MH - Cations/administration & dosage/chemistry MH - Cell Line MH - Electrophoretic Mobility Shift Assay MH - *Gene Transfer Techniques MH - Genetic Vectors MH - Humans MH - Molecular Weight MH - Polyethyleneimine/*administration & dosage/chemistry MH - Polymers/*administration & dosage/chemistry MH - RNA, Small Interfering/administration & dosage/*genetics MH - Thiophenes/*administration & dosage/chemistry MH - Transfection PMC - PMC4619845 EDAT- 2015/11/06 06:00 MHDA- 2016/08/19 06:00 PMCR- 2015/10/11 CRDT- 2015/11/06 06:00 PHST- 2015/04/04 00:00 [received] PHST- 2015/06/13 00:00 [revised] PHST- 2015/06/23 00:00 [accepted] PHST- 2015/11/06 06:00 [entrez] PHST- 2015/11/06 06:00 [pubmed] PHST- 2016/08/19 06:00 [medline] PHST- 2015/10/11 00:00 [pmc-release] AID - 10.1155/2015/406389 [doi] PST - ppublish SO - Biomed Res Int. 2015;2015:406389. doi: 10.1155/2015/406389. Epub 2015 Oct 11.