Key Laboratory of Biotechnology and Bioresources Utilization, Ministry of Education, Dalian Minzu University, Dalian 116600, China.
Key Laboratory of Biotechnology and Bioresources Utilization, Ministry of Education, Dalian Minzu University, Dalian 116600, China.
Adv Colloid Interface Sci. 2018 Mar;253:117-140. doi: 10.1016/j.cis.2017.12.006. Epub 2017 Dec 26.
Cationic lipids have become known as one of the most versatile tools for the delivery of DNA, RNA and many other therapeutic molecules, and are especially attractive because they can be easily designed, synthesized and characterized. Most of cationic lipids share the common structure of cationic head groups and hydrophobic portions with linker bonds between both domains. The linker bond is an important determinant of the chemical stability and biodegradability of cationic lipid, and further governs its transfection efficiency and cytotoxicity. Based on the structures of linker bonds, they can be grouped into many types, such as ether, ester, amide, carbamate, disulfide, urea, acylhydrazone, phosphate, and other unusual types (carnitine, vinyl ether, ketal, glutamic acid, aspartic acid, malonic acid diamide and dihydroxybenzene). This review summarizes some research results concerning the nature (such as the structure and orientation of linker groups) and density (such as the spacing and the number of linker groups) of linker bond for improving the chemical stability, biodegradability, transfection efficiency and cytotoxicity of cationic lipid to overcome the critical barriers of in vitro and in vivo transfection.
阳离子脂质已成为递送 DNA、RNA 和许多其他治疗分子的最通用工具之一，它们特别有吸引力，因为它们可以很容易地设计、合成和表征。大多数阳离子脂质都具有阳离子头基和疏水区以及连接两者的键的共同结构。连接键是阳离子脂质化学稳定性和生物降解性的重要决定因素，进一步控制其转染效率和细胞毒性。根据连接键的结构，它们可以分为许多类型，如醚、酯、酰胺、氨基甲酸酯、二硫键、脲、酰腙、磷酸和其他不常见的类型（肉碱、乙烯醚、缩酮、谷氨酸、天冬氨酸、丙二酸二酰胺和二羟基苯）。本文综述了一些关于连接键的性质（如连接基团的结构和取向）和密度（如连接基团的间隔和数量）的研究结果，以提高阳离子脂质的化学稳定性、生物降解性、转染效率和细胞毒性，克服体外和体内转染的关键障碍。
