Abstract
Knowledge of the mechanism of action of skin penetration enhancers is essential to formulators for optimizing formulations and to maximize the efficacy of enhancers. To obtain information about the effects of penetration enhancers as a fast initial screening, investigations have been performed to identify possible correlations of the biological effectiveness of penetration enhancers with their interaction with a well-defined model system consisting of skin mimic lipid bilayers, as determined by calcein release experiments using stratum corneum lipid liposomes (SCLLs). We aimed to investigate the enhancing effects of different concentrations of two chemical penetration enhancers, Kolliphor RH40 and Transcutol on SCLLs. The results obtained by SCLL-based techniques were compared with conventional ex vivo penetration studies in case of Kolliphor RH40 to evaluate the potential of SCLLs as an alternative tool for screening various types and concentrations of penetration enhancers. As a result, calcein leakage assay performed with SCLL was considered to be a good model for the skin penetration enhancing effect. This method could be used as a time-saving and sensitive alternative in vitro screening technique in the early stage of the development of dermal formulations.
Highlights
The skin has been recognized as a highly attractive application site of therapeutic agents with both local and systemic effects.[1]
The effect of different concentrations of Kolliphor RH40 and Transcutol was tested on the disruption of stratum corneum lipid liposomes (SCLLs) applying calcein leakage assay
Most chemical penetration enhancers act upon the skin by permeabilizing the lipid bilayer membranes in the stratum corneum
Summary
The skin has been recognized as a highly attractive application site of therapeutic agents with both local and systemic effects.[1]. Stratum corneum lipid liposomes (SCLLs) are composed of a lipid mixture approximating the composition of the SC: ceramides (40%), cholesterol (25%), cholesteryl sulfate (10%) and free fatty acids (25%) This lipid composition is capable of forming unilamellar bilayers at physiological pH, and they were shown to be really stable.[4,5] These systems can be applied as in vitro models for screening agents of pharmaceutical or cosmetic interest, enabling the evaluation of their interactions with the permeability barrier.[5] by changing the lipid composition of SCLLs, different pathological conditions can be modelled, e.g. the accumulation of cholesterol sulfate and decreased cholesterol levels are speci c for ichthyosis patients.[6]
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