Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids
The measurement of skin electrical resistance (SER) has drawn a great deal of attention for the rapid screening of transdermal penetration enhancers (PEs). However, the mechanisms underlying the SER measurement are still unclear. This study was to investigate the effects and mechanisms of seven oxyg...
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MDPI AG
2019-01-01
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author | Xue-min Zhu Yu Li Fei Xu Wei Gu Guo-jun Yan Jie Dong Jun Chen |
author_facet | Xue-min Zhu Yu Li Fei Xu Wei Gu Guo-jun Yan Jie Dong Jun Chen |
author_sort | Xue-min Zhu |
collection | DOAJ |
description | The measurement of skin electrical resistance (SER) has drawn a great deal of attention for the rapid screening of transdermal penetration enhancers (PEs). However, the mechanisms underlying the SER measurement are still unclear. This study was to investigate the effects and mechanisms of seven oxygen-containing terpenes on the SER kinetics. Stratum corneum (SC) lipids were proved to play a key role in SER measurement. Then, the factors affecting the SER measurement were optimized. By the determination of SER kinetics, cyclic terpenes (1,8-cineole, terpinen-4-ol, menthol and α-terpineol) were demonstrated to possess higher enhancement ratio (ER) values compared with linear terpenes (linalool, geraniol and citral). For the first time, the linear correlation was found between ER of terpenes and the interaction energy of terpene⁻ceramide complexes revealed by molecular simulation. The attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) analysis revealed that the effect of cyclic terpenes on SC lipid arrangement was obviously stronger than that of linear terpenes. In addition, by evaluating HaCaT skin cell viability, little difference was found between the toxicities of cyclic and linear terpenes. In conclusion, measurement of SER could be a feasible approach for the efficient evaluation of the PEs that mainly act on SC lipids. |
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spelling | doaj.art-31cbe238638348c38777de723c5f3e482022-12-22T03:45:49ZengMDPI AGMolecules1420-30492019-01-0124352310.3390/molecules24030523molecules24030523Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum LipidsXue-min Zhu0Yu Li1Fei Xu2Wei Gu3Guo-jun Yan4Jie Dong5Jun Chen6Pharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaPharmaceutical Research Laboratory, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, ChinaThe measurement of skin electrical resistance (SER) has drawn a great deal of attention for the rapid screening of transdermal penetration enhancers (PEs). However, the mechanisms underlying the SER measurement are still unclear. This study was to investigate the effects and mechanisms of seven oxygen-containing terpenes on the SER kinetics. Stratum corneum (SC) lipids were proved to play a key role in SER measurement. Then, the factors affecting the SER measurement were optimized. By the determination of SER kinetics, cyclic terpenes (1,8-cineole, terpinen-4-ol, menthol and α-terpineol) were demonstrated to possess higher enhancement ratio (ER) values compared with linear terpenes (linalool, geraniol and citral). For the first time, the linear correlation was found between ER of terpenes and the interaction energy of terpene⁻ceramide complexes revealed by molecular simulation. The attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) analysis revealed that the effect of cyclic terpenes on SC lipid arrangement was obviously stronger than that of linear terpenes. In addition, by evaluating HaCaT skin cell viability, little difference was found between the toxicities of cyclic and linear terpenes. In conclusion, measurement of SER could be a feasible approach for the efficient evaluation of the PEs that mainly act on SC lipids.https://www.mdpi.com/1420-3049/24/3/523oxygen-containing terpenespenetration enhancersstratum corneum lipidsskin electrical resistance |
spellingShingle | Xue-min Zhu Yu Li Fei Xu Wei Gu Guo-jun Yan Jie Dong Jun Chen Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids Molecules oxygen-containing terpenes penetration enhancers stratum corneum lipids skin electrical resistance |
title | Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids |
title_full | Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids |
title_fullStr | Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids |
title_full_unstemmed | Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids |
title_short | Skin Electrical Resistance Measurement of Oxygen-Containing Terpenes as Penetration Enhancers: Role of Stratum Corneum Lipids |
title_sort | skin electrical resistance measurement of oxygen containing terpenes as penetration enhancers role of stratum corneum lipids |
topic | oxygen-containing terpenes penetration enhancers stratum corneum lipids skin electrical resistance |
url | https://www.mdpi.com/1420-3049/24/3/523 |
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