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Polymers 2018, 10(10), 1060;

Synthesis and Properties of Low-Molecular-Weight PEI-Based Lipopolymers for Delivery of DNA

National Demonstration Center for Experimental Chemical Engineering Comprehensive Education, School of Chemical Engineering and Technology, North University of China, Taiyuan 030000, China
Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, China
Authors to whom correspondence should be addressed.
Received: 20 August 2018 / Revised: 22 September 2018 / Accepted: 22 September 2018 / Published: 25 September 2018
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Rapid enzymatic degradation and fragmentation during DNA administration can result in limited gene expression, and consequently, poor efficacy. It is necessary to use novel vectors for DNA delivery. Herein, we aimed to design useful carriers for enhancing transfection efficiency (TE). These lipopolymers were prepared through Michael addition reactions from low-molecular-weight (LMW) polyethyleneimine (PEI) and linkers with three kinds of steroids. Agarose gel electrophoresis assay results displayed that the three lipopolymers could condense plasmid DNA well, and the formed polyplexes had appropriate sizes around 200–300 nm, and zeta potentials of about +25–40 mV. The results of in vitro experiments using HeLa, HEK293, and MCF-7 cells showed that these lipopolymers present higher TE than 25-kDa PEI, both in the absence and presence of 10% serum. Flow cytometry and confocal microscopy studies also demonstrated that these lipopolymer/DNA complexes present higher cellular uptake and intracellular distribution. The measurement of critical micelle concentration (CMC) revealed that these lipopolymers could form micelles, which are suited for drug delivery. All results suggest that the three materials may serve as hopeful candidates for gene and drug delivery in future in vivo applications. View Full-Text
Keywords: gene vectors; Michael addition; lipopolymers; steroids gene vectors; Michael addition; lipopolymers; steroids

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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 (CC BY 4.0).

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Xun, M.-M.; Huang, Z.; Xiao, Y.-P.; Liu, Y.-H.; Zhang, J.; Zhang, J.-H.; Yu, X.-Q. Synthesis and Properties of Low-Molecular-Weight PEI-Based Lipopolymers for Delivery of DNA. Polymers 2018, 10, 1060.

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