Amphiphilic and biodegradable hy-PEI-g-PCL-b-PEG copolymers efficiently mediate transgene expression depending on their graft density

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• 作者：Mengyao Zheng¹ ; Yu Liu¹ ; Olga Samsonova¹ ; Thomas Endres ; Olivia Merkel ; Thomas Kissel ; ^{kissel@staff.uni-marburg.de}
• 关键词：Transfection ; Non-viral gene delivery ; Biodegradable copolymer ; Hyper-branched poly(ethylene imine) (hyPEI) ; Graft density ; Buffer-capacity
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：1 May, 2012
• 卷：427
• 期：1
• 页码：80-87
• 文件大小：1638 K

摘要

Novel biodegradable amphiphilic copolymers hy-PEI-g-PCL-b-PEG were prepared by grafting PCL-b-PEG chains onto hyper-branched poly(ethylene imine) as non-viral gene delivery vectors. Our investigations focused on the influence of graft densities of PCL-b-PEG chains on physico-chemical properties, DNA complexation and transfection efficiency. We found that the transfection efficiencies of these polymers increased at first towards an optimal graft density (n = 3) and then decreased. The buffer-capacity-test showed almost exactly the same tendency as transfection efficiency. Cytotoxicity (MTT-assay) depended on the cooperation of PEG molecular weight and graft density of PCL-b-PEG chains. With increasing the graft density, cytotoxicity, zeta-potential, affinity with DNA, stability of the polyplexes and CMC-values were reduced strongly and regularly. Increasing the excess of polymer over DNA was shown to result in a decrease of the observed particle size to 100-200 nm.