title: The headgroup evolution of cationic lipids for gene delivery.
abstract: Cationic lipids are one of the most widely used nonviral vectors for gene delivery and are especially attractive because they can be easily synthesized and extensively characterized. Additionally, they can best facilitate the elucidation of structure-activity relationships by modifying each of their constituent domains. The polar hydrophilic headgroups enable the condensation of nucleic acids by electrostatic interactions with the negatively charged phosphate groups of the genes, and further govern transfection efficiency. The headgroups of cationic lipids play a crucial role for gene delivery; they can be quaternary ammoniums, amines, aminoacids or peptides, guanidiniums, heterocyclic headgroups, and some unusual headgroups. This review summarizes recent research results concerning the nature (such as the structure and shape of cationic headgroup) and density (such as the number and the spacing of cationic headgroup) of head functional groups for improving the design of efficient cationic lipids to overcome the critical barriers of in vitro and in vivo transfection.
authors: State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012, China.
authors: Defu
authors: D
authors: Zhi
authors: Shubiao
authors: S
authors: Zhang
authors: Shaohui
authors: S
authors: Cui
authors: Yinan
authors: Y
authors: Zhao
authors: Yinhuan
authors: Y
authors: Wang
authors: Defeng
authors: D
authors: Zhao
mesh_terms: D002412:Cations / Q000737:chemistry; D018014:Gene Transfer Techniques; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D015394:Molecular Structure
chemical_list: D002412:Cations; D008055:Lipids