title: Investigation of the protonation state of novel cationic lipids designed for gene transfection.
abstract: In order to be used in versatile DNA delivery systems, novel cationic lipids were synthesized. The head groups of the new compounds represented by monoamines or oligoamines can be charged or uncharged depending on the environmental pH. Since their pK values are unknown, the protonation properties of these lipids have been studied in a wide pH range. In our experiments, the amphiphilic molecules were organized as a Langmuir monolayer at the air-water interface. Total reflection X-ray fluorescence (TRXF) was used to determine the 2D concentration of bromide counterions bound to a positively charged (protonated) Langmuir monolayer. The protonation rate of the novel cationic lipids was estimated by comparing the fluorescence intensity with that of dioctadecyldimethylammonium bromide monolayers as a reference. TRXF investigations were supplemented with results of film-balance measurements, grazing incidence X-ray diffraction, and X-ray reflectivity data. The results obtained display that the monolayers of all studied compounds are completely uncharged at pH values above 10. In the investigated pH region, the highest protonation rate of the monolayers is observed at pH 3. The influence of the monolayer packing density on the protonation properties is clearly shown.
authors.affiliation: Max Planck Institute of Colloids and Interfaces, Research Campus Golm, Am Muehlenberg 1, D-14476 Potsdam, Germany. maria.antipina@mpikg.mpg.de
authors.forename: Maria N
authors.initials: MN
authors.lastname: Antipina
authors.forename: Bodo
authors.initials: B
authors.lastname: Dobner
authors.forename: Oleg V
authors.initials: OV
authors.lastname: Konovalov
authors.forename: Vladimir L
authors.initials: VL
authors.lastname: Shapovalov
authors.forename: Gerald
authors.initials: G
authors.lastname: Brezesinski
mesh_terms: D002412:Cations; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011522:Protons; D013050:Spectrometry, Fluorescence; D021241:Spectrometry, Mass, Electrospray Ionization; D014162:Transfection / Q000379:methods*; D014965:X-Rays
chemical_list: D002412:Cations; D008055:Lipids; D011522:Protons