PMID- 27213305 OWN - NLM STAT- MEDLINE DCOM- 20170417 LR - 20200225 IS - 1420-3049 (Electronic) IS - 1420-3049 (Linking) VI - 21 IP - 5 DP - 2016 May 18 TI - Low-Molecular Weight Polyethylenimine Modified with Pluronic 123 and RGD- or Chimeric RGD-NLS Peptide: Characteristics and Transfection Efficacy of Their Complexes with Plasmid DNA. LID - 10.3390/molecules21050655 [doi] LID - 655 AB - To solve the problem of transfection efficiency vs. cytotoxicity and tumor-targeting ability when polyethylenimine (PEI) was used as a nonviral gene delivery vector, new degradable PEI polymers were synthesized via cross-linking low-molecular-weight PEI with Pluronic P123 and then further coupled with a targeting peptide R4 (RGD) and a bifunctional R11 (RGD-NLS), which were termed as P123-PEI-R4 and P123-PEI-R11, respectively. Agarose gel electrophoresis showed that both P123-PEI-R4 and P123-PEI-R11 efficaciously condense plasmid DNA at a polymer-to-pDNA w/w ratio of 3.0 and 0.4, respectively. The polyplexes were stable in the presence of serum and could protect plasmid DNA against DNaseI. They had uniform spherical nanoparticles with appropriate sizes around 100-280 nm and zeta-potentials about +40 mV. Furthermore, in vitro experiments showed that these polyplexes had lower cytotoxicity at any concentration compared with PEI 25 kDa, thus giving promise to high transfection efficiency as compared with another P123-PEI derivate conjugated with trifunctional peptide RGD-TAT-NLS (P123-PEI-R18). More importantly, compared with the other polymers, P123-PEI-R11 showed the highest transfection efficiency with relatively lower cytotoxicity at any concentration, indicating that the new synthetic polymer P123-PEI-R11 could be used as a safe and efficient gene deliver vector. FAU - Hu, Jing AU - Hu J AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. 15821787592@163.com. FAU - Zhao, Wenfang AU - Zhao W AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. wfzhao0504@163.com. FAU - Liu, Kehai AU - Liu K AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. khliu@shou.edu.cn. FAU - Yu, Qian AU - Yu Q AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. 15001970365@163.com. FAU - Mao, Yuan AU - Mao Y AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. 13262975153@163.com. FAU - Lu, Zeyu AU - Lu Z AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. m18701881332@163.com. FAU - Zhang, Yaguang AU - Zhang Y AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. edwarddo@163.com. FAU - Zhu, Manman AU - Zhu M AD - Department of Biopharmaceutics, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, China. zhu_manman7526@163.com. LA - eng PT - Journal Article DEP - 20160518 PL - Switzerland TA - Molecules JT - Molecules (Basel, Switzerland) JID - 100964009 RN - 0 (Nuclear Localization Signals) RN - 0 (Oligopeptides) RN - 0 (Polymers) RN - 147336-22-9 (Green Fluorescent Proteins) RN - 78VO7F77PN (arginyl-glycyl-aspartic acid) RN - 9002-98-6 (Polyethyleneimine) RN - 9007-49-2 (DNA) SB - IM MH - DNA MH - Electrophoresis, Agar Gel MH - *Gene Transfer Techniques MH - Genetic Therapy/*methods MH - Green Fluorescent Proteins MH - HeLa Cells MH - Humans MH - Molecular Weight MH - Nanoparticles/chemistry/therapeutic use MH - Nuclear Localization Signals/chemistry/*genetics/therapeutic use MH - Oligopeptides/chemistry/*genetics/therapeutic use MH - Plasmids/chemistry/genetics MH - Polyethyleneimine/*chemistry/therapeutic use MH - Polymers/chemistry/therapeutic use MH - Transfection/methods PMC - PMC6273895 OTO - NOTNLM OT - RGD OT - nuclear localization signal OT - physico-chemical properties OT - polycations OT - transfection efficiency COIS- The authors declare no conflict of interest. EDAT- 2016/05/24 06:00 MHDA- 2017/04/18 06:00 PMCR- 2016/05/18 CRDT- 2016/05/24 06:00 PHST- 2016/02/22 00:00 [received] PHST- 2016/05/12 00:00 [revised] PHST- 2016/05/13 00:00 [accepted] PHST- 2016/05/24 06:00 [entrez] PHST- 2016/05/24 06:00 [pubmed] PHST- 2017/04/18 06:00 [medline] PHST- 2016/05/18 00:00 [pmc-release] AID - molecules21050655 [pii] AID - molecules-21-00655 [pii] AID - 10.3390/molecules21050655 [doi] PST - epublish SO - Molecules. 2016 May 18;21(5):655. doi: 10.3390/molecules21050655.