O/W emulsion and W/O/W multiple emulsion: physical characterization and skin pharmacokinetic comparison in the delivery process of caffeine

The aim of this study was to compare the characteristics of an O/W emulsion and a W/O/W emulsion, formulated with similar ingredients. The physical properties of these two types of vehicles were characterized first. Using three types of in vitro models, human skin biopsies, nitrate acetate cellulose membranes and human reconstituted epidermis, the delivery potential of each vehicle for one hydrophilic drug, caffeine, was compared. The assessment of physical parameters, such as particle size, conductivity and rheological behavior enabled the nature of the test emulsions to be clearly identified. Clear differences were observed in the ability of each type of emulsion to deliver caffeine. Whatever the nature of the membrane used for the pharmacokinetic study, the absorption of caffeine was roughly two-fold lower (2.6 for human skin) when the W/O/W multiple emulsion was used as the vehicle. The concomitant determination of physical and kinetic properties of these two test emulsions allowed the W/O/W multiple emulsion and a simple O/W emulsion to be clearly differentiated.