核酸疗法是目前治疗肿瘤和遗传疾病以及预防传染病最有前途的方法。然而,这种治疗的最大障碍是将核酸递送到靶位点,这需要克服免疫系统捕获等问题,需要穿透生物膜,和核酸性能的退化。设计合适的递送载体是解决这些问题的关键。脂质-由亲水头基组成,链接器,和疏水尾部是构建载体的关键组成部分。头组特别重要,因为它影响药物包封率,载体的细胞毒性,和转染效率。在这里,我们专注于各种头基结构(叔胺,季铵盐,肽,哌嗪,树枝状聚合物,和其他几个),并对近年来发展起来的重要脂质载体进行了总结和分类。我们还讨论了具有各种头基团的阳离子脂质在核酸药物递送中的应用,并分析了头基结构如何影响运输效率和载体毒性。最后,我们简要描述了开发新型脂质载体的挑战,以及他们的前景。
Nucleic acid therapy is currently the most promising method for treating tumors and genetic diseases and for preventing infectious diseases. However, the biggest obstacle to this therapy is delivery of the nucleic acids to the target site, which requires overcoming problems such as capture by the immune system, the need to penetrate biofilms, and degradation of nucleic acid performance. Designing suitable delivery vectors is key to solving these problems. Lipids-which consist of a hydrophilic headgroup, a linker, and a hydrophobic tail-are crucial components for the construction of vectors. The headgroup is particularly important because it affects the drug encapsulation rate, the vector cytotoxicity, and the transfection efficiency. Herein, we focus on various headgroup structures (tertiary amines, quaternary ammonium salts, peptides, piperazines, dendrimers, and several others), and we summarize and classify important lipid-based carriers that have been developed in recent years. We also discuss applications of cationic lipids with various headgroups for delivery of nucleic acid drugs, and we analyze how headgroup structure affects transport efficiency and carrier toxicity. Finally, we briefly describe the challenges of developing novel lipid carriers, as well as their prospects.