PMID- 23184839 OWN - NLM STAT- MEDLINE DCOM- 20130625 LR - 20201209 IS - 2192-2640 (Print) IS - 2192-2640 (Linking) VI - 2 IP - 3 DP - 2013 Mar TI - PEGylated peptide based reductive polycations as efficient nonviral gene vectors. PG - 481-9 LID - 10.1002/adhm.201200154 [doi] AB - To overcome the critical barriers in gene delivery, a series of reducible polycations (RPCs) based on low molecular weight (LMW) peptides, i.e. PolyHK6 H, PolyHK6 H-mPEG1 , PolyHK6 H-mPEG2 , and PolyHK6 H-mPEG3 , with different poly(ethylene glycol) (PEG) contents, are synthesized and evaluated as nonviral gene vectors. All the RPCs exhibit lower cytotoxicity compared with 25 kDa polyethyleneimine (PEI) and PEGylated PEI (PEI-mPEG: PEI-mPEG1 , PEI-mPEG2 , and PEI-mPEG3 ). PolyHK6 H-mPEG1 and PolyHK6 H-mPEG2 can bind and condense plasmid deoxyribonucleic acid (pDNA) efficiently with a particle size of about 200 nm. Moreover, they display much higher transfection efficiency than that of 25 kDa PEI especially in serum-supplemented medium. Moreover, PolyHK6 H-mPEG1 has equal transfection efficiency with PEI-mPEG1 which is optimal in the PEI-mPEG, but PolyHK6 H-mPEG1 exhibits significantly lower cytotoxicity than PEI-mPEG1 . This is attributed to the fact that inter-peptide disulfide bonds can increase the stability of RPCs/pDNA complexes in extracellular environment and thereafter cleave in cytoplasm to facilitate the release of pDNA in intracellular environment. The PEGylated RPCs demonstrate here improved intracellular gene transfer performance and will have great potential applications in vivo. CI - Copyright (c) 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. FAU - Yang, Juan AU - Yang J AD - Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, China. FAU - Wang, Hui-Yuan AU - Wang HY FAU - Yi, Wen-Jie AU - Yi WJ FAU - Gong, Yu-Hui AU - Gong YH FAU - Zhou, Xiang AU - Zhou X FAU - Zhuo, Ren-Xi AU - Zhuo RX FAU - Zhang, Xian-Zheng AU - Zhang XZ LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20121004 PL - Germany TA - Adv Healthc Mater JT - Advanced healthcare materials JID - 101581613 RN - 0 (Drug Carriers) RN - 0 (Peptides) RN - 0 (Polyamines) RN - 0 (Polyelectrolytes) RN - 0 (polycations) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 9007-49-2 (DNA) SB - IM MH - Animals MH - COS Cells MH - Chlorocebus aethiops MH - DNA/chemistry/genetics/*pharmacokinetics MH - Drug Carriers/chemistry MH - Drug Stability MH - Electrophoretic Mobility Shift Assay MH - *Gene Transfer Techniques MH - Genetic Vectors/*chemistry MH - HeLa Cells MH - Humans MH - Microscopy, Fluorescence MH - Particle Size MH - Peptides/*chemistry MH - Polyamines/*chemistry MH - Polyelectrolytes MH - Polyethylene Glycols/*chemistry EDAT- 2012/11/28 06:00 MHDA- 2013/06/26 06:00 CRDT- 2012/11/28 06:00 PHST- 2012/05/10 00:00 [received] PHST- 2012/08/28 00:00 [revised] PHST- 2012/11/28 06:00 [entrez] PHST- 2012/11/28 06:00 [pubmed] PHST- 2013/06/26 06:00 [medline] AID - 10.1002/adhm.201200154 [doi] PST - ppublish SO - Adv Healthc Mater. 2013 Mar;2(3):481-9. doi: 10.1002/adhm.201200154. Epub 2012 Oct 4.