title: Biotinylated cyclen-contained cationic lipids as non-viral gene delivery vectors.
abstract: A series of 1, 4, 7, 10-tetraazacyclododecane (cyclen)-based cationic lipids, namely 5a-c bearing a biotin moiety and a variety of end groups (cholesterol, diosgenin, and α-tocopherol) via biodegradable carbamate bond linkage were prepared and applied as non-viral gene delivery vectors. The liposomes formed from 5 and dioleoylphosphatidylethanolamine could bind and condense plasmid DNA into nanoparticles with appropriate size and zeta potentials. All biotinylated cyclen cationic lipids showed higher cell viability than commercially available lipofectamine 2000 even at high N/P ratios, while their transfection efficiency was relatively lower. Further, results indicate that among the three lipids, α-tocopherol-containing compound 5c has higher DNA-binding ability, lower cytotoxicity, and higher transfection efficiency. Transfection in two different cell lines revealed that these lipoplexes have higher gene delivery efficiency toward tumor cells.
authors: Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, 610064, China.
authors: Qiang
authors: Q
authors: Liu
authors: Wen-Jing
authors: WJ
authors: Yi
authors: Yi-Mei
authors: YM
authors: Zhang
authors: Ji
authors: J
authors: Zhang
authors: Liandi
authors: L
authors: Guo
authors: Xiao-Qi
authors: XQ
authors: Yu
mesh_terms: D001710:Biotin / Q000737:chemistry*; D002412:Cations; D045744:Cell Line, Tumor; D000080027:Cyclams; D005822:Genetic Vectors; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D010957:Plasmids; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D002412:Cations; D000080027:Cyclams; D006571:Heterocyclic Compounds; D008055:Lipids; D001710:Biotin; C038072:cyclen
keywords: biotin; cationic lipid; cyclen; gene delivery; non-viral vector