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. 2018 Aug 2;8(48):27464-27469.
doi: 10.1039/c8ra04129f. eCollection 2018 Jul 30.

Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

Mónika Bakonyi  1 , Attila Gácsi  1 , Szilvia Berkó  1 , Anita Kovács  1 , Erzsébet Csányi  1
Affiliations

Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

Mónika Bakonyi et al. RSC Adv. .

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.

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Conflict of interest statement

There are no conflicts to declare.

Figures

Fig. 1
Fig. 1. Transmission electron microscope images of SCLLs (A) and calcein-loaded SCLLs (B).
Fig. 2
Fig. 2. Efflux from SCLLs induced by Kolliphor RH40 (A) and Transcutol (B) as a function of incubation time. The concentrations of the CPEs are indicated in the plot.
Fig. 3
Fig. 3. Calcein efflux from SCLLs after 1 h of incubation as a function of CPE concentration (▲: Kolliphor RH40, ●: Transcutol).
Fig. 4
Fig. 4. Calcein efflux as a function of the entrapped fluorescence lifetime on a reciprocal scale brought on by Kolliphor RH40 (A) and Transcutol (B).
Fig. 5
Fig. 5. Cumulative amount of caffeine penetrated through heat separated epidermis after application of different concentrations of Kolliphor RH40.
Fig. 6
Fig. 6. Relationship between calcein leakage and increase in the caffeine permeated compared to blank formulation after 1 and 2 hours.
See this image and copyright information in PMC

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