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Integration of Polylactide into Polyethylenimine Facilitates the Safe and Effective Intracellular siRNA Delivery

by Guo-Bin Ding 1,2,*, Xue Meng 1,2, Peng Yang 1,2, Binchun Li 1, Roland H Stauber 1,3 and Zhuoyu Li 1,2,*
1
Institute of Biotechnology, the Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Shanxi University, Taiyuan 030006, China
2
Institutes of Biomedical Sciences, Shanxi University, Taiyuan 030006, China
3
Molecular and Cellular Oncology, University Medical Center Mainz, Langenbeckstrasse 1, 55101 Mainz, Germany
*
Authors to whom correspondence should be addressed.
Polymers 2020, 12(2), 445; https://doi.org/10.3390/polym12020445 (registering DOI)
Received: 18 December 2019 / Revised: 31 January 2020 / Accepted: 11 February 2020 / Published: 14 February 2020
(This article belongs to the Section Polymer Applications)
Polyethylenimine (PEI) is a gold standard polymer with excellent transfection efficacy, yet its severe toxicity and nondegradability hinders its therapeutic application as a gene delivery vector. To tackle this problem, herein we incorporated the biodegradable polylactide (PLA) into the branched PEI by synthesizing a PEI-PLA copolymer via a facile synthetic route. PLA modification significantly improved the cytocompatibility of PEI, PEI-PLA copolymer showed much higher cell viability than PEI as verified in three different human cancer cell lines (HCT116, HepG2 and SKOV3). Interestingly, the PEI-PLA copolymer could effectively bind siRNA targeting PKM2, and the obtained polyplex displayed much higher stability in serum than naked siRNA as determined by agarose gel electrophoresis. Moreover, cellular uptake study demonstrated that PEI-PLA could efficiently deliver the Cy5-labled siRNA into the three tested cancer cell lines, and the transfection efficiency is equivalent to the commercial Lipofectamine® 2000. Finally, it is noteworthy that the polyplex is comparable to Lipo2000 in down-regulating the expression of PKM2 at both mRNA and protein level as measured by q-PCR and western blotting, respectively. Overall, the PEI-PLA copolymer developed in this study has the potential to be developed as a versatile carrier for safe and effective delivery of other nucleic acid-based agents. View Full-Text
Keywords: PEI-PLA copolymer; siRNA targeting PKM2; serum stability; cytotoxicity; transfection efficiency PEI-PLA copolymer; siRNA targeting PKM2; serum stability; cytotoxicity; transfection efficiency
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Ding, G.-B.; Meng, X.; Yang, P.; Li, B.; Stauber, R.H.; Li, Z. Integration of Polylactide into Polyethylenimine Facilitates the Safe and Effective Intracellular siRNA Delivery. Polymers 2020, 12, 445.

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