【摘 要】
：
To solve the problem of transfection efficiency versus cytotoxicity and tumor-targeting ability when polyethylenimine (PEI) was used as a nonviral gene delivery vector,new degradable PEI polymers were
【机 构】
：
College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306,China
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To solve the problem of transfection efficiency versus 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 P123-PEI-R11 respectively.Agarose gel electrophoresis showed that both P123-PEI-R4 and P123-PEI-Rll 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 DNase I.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-Rll could be used as a safe and efficient gene deliver vector.
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