title: Preparation, characterization, transfection efficiency, and cytotoxicity of liposomes containing oligoamine-modified cholesterols as nanocarriers to Neuro2A cells.
abstract: In the present study, three derivatives of cholesterol that contain an amino head group with a different spacer arm were synthesized. A novel gene delivery system was developed using liposomes composed of DOTAP and oligoamines-modified cholesterol. These multilamellar vesicle (MLV) liposomes were extruded through 400- and 100-nm polycarbonate filters to produce large unilamellar vesicles (LUVs). Transfection efficiency in Neuro2A cells was tested using plasmid DNA encoding Renilla luciferase, and the cytotoxicity of the prepared lipoplexes was also evaluated. LUV liposomes containing derivative III showed the highest transfection efficiency among other synthesized derivatives, but among MLV liposomes, cationic liposomes with derivative I had the best transfection activity. In all cases, transfection increased by increasing the ratio of cationic lipid to DNA. Almost all formulations were not cytotoxic on Neuro2A cells. The results indicated that the designed systems are able to transfer the DNA into Neuro2A cells with low or no toxicity.
  
  
  BACKGROUND
  This study describes the ideal parameters for preparing large unilamellar vesicles as nanocarriers containing oligoamine-modified cholesterols. The results indicated that the designed systems are able to transfer the DNA into Neuro2A cells with low or no toxicity.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Research Centre, Mashhad University of Medical Sciences, Mashhad, Iran.
authors.forename: Bizhan
authors.initials: B
authors.lastname: Malaekeh-Nikouei
authors.forename: Mohammad
authors.initials: M
authors.lastname: Malaekeh-Nikouei
authors.forename: Reza Kazemi
authors.initials: RK
authors.lastname: Oskuee
authors.forename: Mohammad
authors.initials: M
authors.lastname: Ramezani
mesh_terms: D000588:Amines / Q000378:metabolism*; D000818:Animals; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D002784:Cholesterol / Q000737:chemistry / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D004952:Esters / Q000737:chemistry; D004996:Ethidium; D006801:Humans; D008081:Liposomes / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D014162:Transfection
chemical_list: D000588:Amines; D004337:Drug Carriers; D004952:Esters; D008081:Liposomes; D002784:Cholesterol; D004996:Ethidium