title: Synthesis, characterization, and in vitro transfection activity of charge-reversal amphiphiles for DNA delivery.
abstract: A series of charge-reversal lipids were synthesized that possess varying chain lengths and end functionalities. These lipids were designed to bind and then release DNA based on a change in electrostatic interaction with DNA. Specifically, a cleavable ester linkage is located at the ends of the hydrocarbon chains. The DNA release from the amphiphile was tuned by altering the length and position of the ester linkage in the hydrophobic chains of the lipids through the preparation of five new amphiphiles. The amphiphiles and corresponding lipoplexes were characterized by DSC, TEM, and X-ray, as well as evaluated for DNA binding and DNA transfection. For one specific charge-reversal lipid, stable lipoplexes of approximately 550 nm were formed, and with this amphiphile, effective in vitro DNA transfection activities was observed.
authors: Departments of Biomedical Engineering and Chemistry, Boston University , Boston, Massachusetts 02215, United States.
authors: Xiao-Xiang
authors: XX
authors: Zhang
authors: Carla A H
authors: CA
authors: Prata
authors: Jason A
authors: JA
authors: Berlin
authors: Thomas J
authors: TJ
authors: McIntosh
authors: Philippe
authors: P
authors: Barthelemy
authors: Mark W
authors: MW
authors: Grinstaff
mesh_terms: D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D045744:Cell Line, Tumor; D006224:Cricetinae; D003412:Cricetulus; D004247:DNA / Q000008:administration & dosage* / Q000737:chemistry / Q000235:genetics; D018014:Gene Transfer Techniques; D057809:HEK293 Cells; D006801:Humans; D008055:Lipids / Q000138:chemical synthesis* / Q000737:chemistry*; D051379:Mice; D015394:Molecular Structure; D014162:Transfection
chemical_list: D008055:Lipids; D004247:DNA