The effect of hydrophilic penetration/diffusion enhancer on stratum corneum lipid models: Part II*: DMSO

Abstract

To optimize dermal and transdermal administration of drugs, the barrier function of the skin, particularly the stratum corneum (SC), needs to be reduced reversibly. For this purpose, penetration/diffusion enhancers such as DMSO can be applied. However, there is the question whether DMSO is an aggressive penetration/diffusion enhancer in pharmaceutical and cosmetical relevant concentrations? Until now, it is unclear if this penetration/diffusion enhancement is caused by an interaction with the SC lipid matrix or related to effects within the corneocytes. Therefore, the effects of the hydrophilic enhancer DMSO on SC models with different dimensionality ranging from bilayers (liposomes) via oligo-layers to multilayers have been investigated in this study. The effects of DMSO should be compared to that of other relevant hydrophilic enhancers such as urea and taurine. An innovative spectrum of methods was applied to ascertain the mode of action of DMSO in relevant concentrations on a molecular scale.The experiments reveal that there is no specific interaction of 10% and 30% DMSO solutions with the SC model systems. Hence, if DMSO is applied in pharmaceutically and cosmetically relevant concentrations, it has no influence on the SC model systems used. Neither an additional water uptake in the head group region nor a decrease of the lipid chain packing density have been observed. The leakage studies on liposomes show that 10% DMSO is causing just a very slight leakage of 8%, lower than the leakage of 19.4% caused by 10% urea (Müller et al., 2016). Consequently, the interactions of DMSO with the SC model lipids used are very low in concentrations of 10% and 30%, respectively. Since the lipid composition in native SC lipid matrix is far more complex than this model mixture, the results can not be directly transferred to the native SC lipid matrix. However, the outcome of this study, together with various findings in the literature give rise to the assumption that the enhancing effect of DMSO concerning the diffusion of relevant hydrophilic drugs and actives appears to be realized via the corneocytes.