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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Main Authors: Xue-min Zhu, Yu Li, Fei Xu, Wei Gu, Guo-jun Yan, Jie Dong, Jun Chen
Format: Article
Language:English
Published: MDPI AG 2019-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/24/3/523
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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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