Laboratory of Organic and Macromolecular Chemistry, Friedrich-Schiller-University Jena, Humboldtstraße 10, 07743 Jena, Germany.
Chem Soc Rev. 2012 Jul 7;41(13):4755-67. doi: 10.1039/c2cs35146c. Epub 2012 May 30.
Poly(ethylene imine)s (PEIs) are widely used in different applications, but most extensively investigated as non-viral vector systems. The high ability of cationic PEIs to complex and condense negatively charged DNA and RNA combined with their inherent proton sponge behavior accounts for the excellent efficiency in gene delivery. Further chemical modifications of the polymer expand the application potential, primarily aiming at increased transfection efficiency, cell selectivity and reduced cytotoxicity. Improvements in the synthesis of tailor-made PEIs in combination with new in-depth analytical techniques offer the possibility to produce highly purified polymers with defined structures. The contemporary strategies towards linear and branched poly(ethylene imine)s with modified surface characteristics, PEI-based copolymers as well as conjugates with bioactive molecules will be discussed. In this regard, the versatile branched PEIs have been successfully modified in a statistical manner, whereas the linear counterparts open avenues to design and synthesize well-defined architectures, in order to exploit their high potential in gene delivery.
聚(亚乙基亚胺)(PEIs)在不同的应用中被广泛使用,但作为非病毒载体系统的研究最为广泛。阳离子聚(亚乙基亚胺)具有与带负电荷的 DNA 和 RNA 复合和凝聚的高能力,加上其固有的质子海绵行为,这解释了其在基因传递方面的优异效率。该聚合物的进一步化学修饰扩展了应用潜力,主要旨在提高转染效率、细胞选择性和降低细胞毒性。与新的深入分析技术相结合的定制化聚(亚乙基亚胺)的合成改进提供了生产具有定义结构的高度纯化聚合物的可能性。本文将讨论具有修饰表面特性的线性和支化聚(亚乙基亚胺)、基于聚(亚乙基亚胺)的共聚物以及与生物活性分子的缀合物的当代策略。在这方面,支化的聚(亚乙基亚胺)已成功地以统计方式进行修饰,而线性对应物则为设计和合成具有明确结构的聚合物开辟了途径,以利用其在基因传递方面的高潜力。