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Article

A Molecular Interpretation on the Different Penetration Enhancement Effect of Borneol and Menthol towards 5-Fluorouracil

by 1,2,†, 1,†, 1,2, 1, 1,2, 1,2,* and 1,2,*
1
Beijing University of Chinese Medicine, No. 11 of North 3rd Ring East Road, Chaoyang District, Beijing 100029, China
2
Key Laboratory of TCM-Information Engineering of State Administration of TCM, No. 11 of North 3rd Ring East Road, Chaoyang District, Beijing 100029, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this study.
Int. J. Mol. Sci. 2017, 18(12), 2747; https://doi.org/10.3390/ijms18122747
Received: 29 September 2017 / Revised: 29 November 2017 / Accepted: 12 December 2017 / Published: 18 December 2017
(This article belongs to the Section Molecular Biophysics)
Borneol and menthol are terpenes that are widely used as penetration enhancers in transdermal drug delivery. To explore their penetration-enhancement effects on hydrophilic drugs, 5-fluorouracil (5-FU) was selected as a model drug. An approach that combined in vitro permeation studies and coarse-grained molecular dynamics was used to investigate their penetration-enhancement effect on 5-FU. The results showed that although both borneol and menthol imparted penetration-enhancement effects on 5-FU, these differed in terms of their mechanism, which may account for the observed variations in penetration-enhancement effects. The main mechanism of action of menthol involves the disruption of the stratum corneum (SC) bilayer, whereas borneol involves multiple mechanisms, including the disruption of the SC bilayer, increasing the diffusion coefficient of 5-FU, and inducing the formation of transient pores. The findings of the present study improve our understanding of the molecular mechanism that is underlying 5-FU penetration-enhancement by borneol and menthol, which may be utilized in future investigations and applications. View Full-Text
Keywords: penetration enhancement; molecular mechanism; coarse-grained molecular dynamics; menthol; borneol; 5-fluorouracil penetration enhancement; molecular mechanism; coarse-grained molecular dynamics; menthol; borneol; 5-fluorouracil
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MDPI and ACS Style

Wang, R.; Wu, Z.; Yang, S.; Guo, S.; Dai, X.; Qiao, Y.; Shi, X. A Molecular Interpretation on the Different Penetration Enhancement Effect of Borneol and Menthol towards 5-Fluorouracil. Int. J. Mol. Sci. 2017, 18, 2747. https://doi.org/10.3390/ijms18122747

AMA Style

Wang R, Wu Z, Yang S, Guo S, Dai X, Qiao Y, Shi X. A Molecular Interpretation on the Different Penetration Enhancement Effect of Borneol and Menthol towards 5-Fluorouracil. International Journal of Molecular Sciences. 2017; 18(12):2747. https://doi.org/10.3390/ijms18122747

Chicago/Turabian Style

Wang, Ran, Zhimin Wu, Shufang Yang, Shujuan Guo, Xingxing Dai, Yanjiang Qiao, and Xinyuan Shi. 2017. "A Molecular Interpretation on the Different Penetration Enhancement Effect of Borneol and Menthol towards 5-Fluorouracil" International Journal of Molecular Sciences 18, no. 12: 2747. https://doi.org/10.3390/ijms18122747

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