A drug-lipid interaction model: Atropine induces interdigitated bilayer structure

X-ray diffraction and fluorescence methods have been carried out to examine the effects of a drug, atropine, on the structure of model membranes: dipalmitoylphosphatidylglycerol(DPPG) multilamella vesicles(MLVs). A structural analysis by small angle x-ray diffraction shows that, with incorporation of atropine, the lamella repeating period of DPPG MLV is decreased from 5.89nm to 4.52nm. Using fluorescence probe 1,6-diphenyl-1,3,5-hexatriene(DPH) we find that the fluorescence intensity of DPH reduces largely at a narrow scope of atropine concentration. The experiments of fluorescence polarization of n-(9-anthroyloxyl)-stearic acid (nAS) and 16-(9-anthroyloxyl)-palmiticacid (16AP) discover that the normal polarization gradient almost disappears in DPPG/atropine system. By colligating the above results, we can draw a conclusion that atropine induces the transition from non-interdigitated to interdigitated stricture of DPPG vesicles in gel phase, which provides a sound model of drug-lipid interaction. (C) 1998 Academic Press.