The role of counterions in the membrane-disruptive properties of pH-sensitive lysine-based surfactants.

摘要: Surfactants are among the most versatile and widely used excipients in pharmaceuticals. This versatility, together with their pH-responsive membrane-disruptive activity low toxicity, could also enable potential application drug delivery systems. Five anionic lysine-based surfactants which differ nature of counterion were studied. Their capacity to disrupt cell membrane was examined under a range pH values, concentrations incubation times, using standard hemolysis assay as model for endosomal membranes. The showed pH-sensitive hemolytic improved kinetics at range. Low resulted negligible physiological high lytic 5.4, is characteristic late endosomes. With increasing concentration, an enhanced lyse membranes, caused significant disruption pH. observation indicates that, concentrations, surfactant behavior independent mechanism surfactant-mediated destabilization addressed, scanning electron microscopy studies performed evaluate effects compounds on erythrocyte morphology function vitro cytotoxicity assessed by MTT NRU assays 3T3 line. influence different types applications these discussed. possibility endosome hold great promise intracellular systems future therapeutic applications.