Preprint Article Version 1 This version is not peer-reviewed

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

Version 1 : Received: 29 September 2017 / Approved: 29 September 2017 / Online: 29 September 2017 (12:39:49 CEST)

A peer-reviewed article of this Preprint also exists.

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. 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.

Journal reference: Int. J. Mol. Sci. 2017, 18, 2747
DOI: 10.3390/ijms18122747

Abstract

Borneol and menthol were two terpenes wildly used as penetrate enhancer in transdermal drug delivery. To explore their penetration enhancement effect towards hydrophilic drug, 5-FU was selected as model drug. A method combined vitro permeation studies and coarse grain molecular dynamics was used to investigate their penetration enhancement effect towards 5-FU. As a result, although both borneol and menthol showed a penetration enhancement effect towards 5-FU, they differed a lot in the penetration enhancement mechanism, which was also thought to account for their different penetration enhancement effect. As for menthol, SC bilayer disrupting effect seemed to be its main mechanism. While for borneol, its mechanism seemed to be more complicated. Except for disrupting the SC bilayer, it could also increase the permeation of 5-FU by enhancing the diffusion rate of 5-FU or inducing the formation of transient pore. All of this   enable us a molecular understanding of borneol and menthol’s penetration enhancement effect towards hydrophilic drug, which might provide some guidance in the latter research and application.

Subject Areas

penetration enhancement effect; molecular mechanism; coarse grain molecular dynamics; menthol; borneol; 5-FU

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