Wen Yuting, Pan Shirong, Luo Xin, Zhang Xuan, Zhang Wei, Feng Min
School of Pharmaceutical Sciences and the First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China.
Bioconjug Chem. 2009 Feb;20(2):322-32. doi: 10.1021/bc800428y.
Polyethylenimine (PEI) is a class of cationic polymers proven to be effective for gene delivery. However, PEI is nondegradable and the molecular weight of PEI affects the cytotoxicity and gene transfer activity. Aiming to prepare a biodegradable gene vector with high transfection efficiency and low cytotoxicity, we conjugated low molecular weight (LMW) PEIs to the biodegradable backbone polyglutamic acids derivative (PEG-b-PBLG) by aminolysis to form PEIs combined PEG-b-PLG-g-PEIs (GGI). Two copolymers, GGI 30 and GGI 40, were synthesized. The chemistry of GGI was characterized using IR, 1H NMR and 13C NMR, GPC, and CD, respectively. The degradation behaviors of copolymer GGI in papain solution were investigated. GGIs showed good DNA condensation ability and high protection of DNA from nuclease degradation. The zeta potential of the GGI/pDNA polyplexes was approximately 15 mV, and the particle size was in the range 102-138 nm at N/P ratios between 10 and 30. The particle size and the morphology of the polyplex was further confirmed by transmission electron microscope (TEM). In cytotoxicity assay, GGIs were significantly less toxic than PEI 25k. The degradation product of GGI exhibited negligible effects on cells even at high copolymer concentration. The results of GFP flow cytometry and fluorescence imaging showed that the trasnfection efficiencies of GGIs were all markedly higher than PEI 25k in Hela, HepG2, Bel 7402, and 293 cell lines. Importantly, the presence of serum had a lower inhibitive effect on the transfection activity of GGI in comparison to PEI 25k and Lipofectamine 2000. Therefore, PEG-b-PLG-g-PEI copolymers may be attractive cationic polymers for nonviral gene therapy.
聚乙烯亚胺(PEI)是一类已被证明对基因传递有效的阳离子聚合物。然而,PEI不可降解,且其分子量会影响细胞毒性和基因转移活性。为了制备一种具有高转染效率和低细胞毒性的可生物降解基因载体,我们通过氨解将低分子量(LMW)PEI与可生物降解主链聚谷氨酸衍生物(PEG-b-PBLG)共轭,形成PEI结合的PEG-b-PLG-g-PEI(GGI)。合成了两种共聚物,GGI 30和GGI 40。分别使用红外光谱(IR)、1H核磁共振(1H NMR)、13C核磁共振(13C NMR)、凝胶渗透色谱(GPC)和圆二色光谱(CD)对GGI的化学结构进行了表征。研究了共聚物GGI在木瓜蛋白酶溶液中的降解行为。GGI表现出良好的DNA凝聚能力以及对DNA免受核酸酶降解的高度保护作用。GGI/pDNA多聚体的zeta电位约为15 mV,在N/P比为10至三十时粒径范围为102 - 138 nm。通过透射电子显微镜(TEM)进一步确认了多聚体的粒径和形态。在细胞毒性测定中,GGI的毒性明显低于PEI 25k。即使在高共聚物浓度下,GGI的降解产物对细胞的影响也可忽略不计。绿色荧光蛋白(GFP)流式细胞术和荧光成像结果表明,在Hela、HepG2、Bel 7402和293细胞系中,GGI的转染效率均明显高于PEI 25k。重要的是,与PEI 25k和Lipofectamine 2000相比,血清的存在对GGI转染活性的抑制作用较低。因此,PEG-b-PLG-g-PEI共聚物可能是用于非病毒基因治疗的有吸引力的阳离子聚合物。
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