Sun Yanping, Yang Zhen, Wang Chunxi, Yang Tianzhi, Cai Cuifang, Zhao Xiaoyun, Yang Li, Ding Pingtian
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Department of Basic Pharmaceutical Sciences, School of Pharmacy, Husson University, Bangor, ME, USA.
Acta Biomater. 2017 Sep 15;60:23-37. doi: 10.1016/j.actbio.2017.07.043. Epub 2017 Aug 1.
Polymers are widely studied as non-viral gene vectors because of their strong DNA binding ability, capacity to carry large payload, flexibility of chemical modifications, low immunogenicity, and facile processes for manufacturing. However, high cytotoxicity and low transfection efficiency substantially restrict their application in clinical trials. Incorporating functional peptides is a promising approach to address these issues. Peptides demonstrate various functions in polymer-based gene delivery systems, such as targeting to specific cells, breaching membrane barriers, facilitating DNA condensation and release, and lowering cytotoxicity. In this review, we systematically summarize the role of peptides in polymer-based gene delivery, and elaborate how to rationally design polymer-peptide based gene delivery vectors.
Polymers are widely studied as non-viral gene vectors, but suffer from high cytotoxicity and low transfection efficiency. Incorporating short, bioactive peptides into polymer-based gene delivery systems can address this issue. Peptides demonstrate various functions in polymer-based gene delivery systems, such as targeting to specific cells, breaching membrane barriers, facilitating DNA condensation and release, and lowering cytotoxicity. In this review, we highlight the peptides' roles in polymer-based gene delivery, and elaborate how to utilize various functional peptides to enhance the transfection efficiency of polymers. The optimized peptide-polymer vectors should be able to alter their structures and functions according to biological microenvironments and utilize inherent intracellular pathways of cells, and consequently overcome the barriers during gene delivery to enhance transfection efficiency.
聚合物因其强大的DNA结合能力、携带大量载荷的能力、化学修饰的灵活性、低免疫原性以及简便的制造工艺而被广泛研究作为非病毒基因载体。然而，高细胞毒性和低转染效率严重限制了它们在临床试验中的应用。掺入功能肽是解决这些问题的一种有前途的方法。肽在基于聚合物的基因递送系统中表现出多种功能，如靶向特定细胞、突破膜屏障、促进DNA凝聚和释放以及降低细胞毒性。在本综述中，我们系统地总结了肽在基于聚合物的基因递送中的作用，并阐述了如何合理设计基于聚合物-肽的基因递送载体。
聚合物作为非病毒基因载体被广泛研究，但存在高细胞毒性和低转染效率的问题。将短的生物活性肽掺入基于聚合物的基因递送系统可以解决这个问题。肽在基于聚合物的基因递送系统中表现出多种功能，如靶向特定细胞、突破膜屏障、促进DNA凝聚和释放以及降低细胞毒性。在本综述中，我们强调了肽在基于聚合物的基因递送中的作用，并阐述了如何利用各种功能肽来提高聚合物的转染效率。优化后的肽-聚合物载体应能够根据生物微环境改变其结构和功能，并利用细胞固有的细胞内途径，从而克服基因递送过程中的障碍以提高转染效率。
