ArticleInternational journal of molecular sciences2016
Effects of Concentrations on the Transdermal Permeation Enhancing Mechanisms of Borneol: A Coarse-Grained Molecular Dynamics Simulation on Mixed-Bilayer Membranes.
Article in International journal of molecular sciences, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 23 citations in OpenAlex.
- Article
- In Silico ADME Methods Used in the Evaluation of Natural Products.Pharmaceutics · 2025Review
- Natural Ingredients of Transdermal Drug Delivery Systems as Permeation Enhancers of Active Substances through theMolecular pharmaceutics · 2023Review
- Using molecular simulation to understand the skin barrier.Progress in lipid research · 2022Review
- Molecular perspective of efficiency and safety problems of chemical enhancers: bottlenecks and recent advances.Drug delivery and translational research · 2022Review
- Recent Progress on the Synergistic Antitumor Effect of a Borneol-Modified Nanocarrier Drug Delivery System.Frontiers in medicine · 2021Review
- Influence of Bile Composition on Membrane Incorporation of Transient Permeability Enhancers.Molecular pharmaceutics · 2020Article
- Finite Element Analysis for Predicting Skin Pharmacokinetics of Nano Transdermal Drug Delivery System Based on the Multilayer Geometry Model.International journal of nanomedicine · 2020Article
- Preparation and in vitro and in vivo Study of Asiaticoside-Loaded Nanoemulsions and Nanoemulsions-Based Gels for Transdermal Delivery.International journal of nanomedicine · 2020Article
- Molecular Dynamics Simulations of Membrane Permeability.Chemical reviews · 2019Review
- A Molecular Interpretation on the Different Penetration Enhancement Effect of Borneol and Menthol towards 5-Fluorouracil.International journal of molecular sciences · 2017Article
- Influence of Temperature on Transdermal Penetration Enhancing Mechanism of Borneol: A Multi-Scale Study.International journal of molecular sciences · 2017Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Borneol is a natural permeation enhancer that is effective in drugs used in traditional clinical practices as well as in modern scientific research. However, its molecular mechanism is not fully understood. In this study, a mixed coarse-grained model of stratum corneum (SC) lipid bilayer comprised of Ceramide-N-sphingosine (CER NS) 24:0, cholesterol (CHOL) and free fatty acids (FFA) 24:0 (2:2:1) was used to examine the permeation enhancing mechanism of borneol on the model drug osthole. We found two different mechanisms that were dependent on concentrations levels of borneol. At low concentrations, the lipid system maintained a bilayer structure. The addition of borneol made the lipid bilayer loosen and improved drug permeation. The "pull" effect of borneol also improved drug permeation. However, for a strongly hydrophobic drug like osthole, the permeation enhancement of borneol was limited. When most borneol molecules permeated into bilayers and were located at the hydrophobic tail region, the spatial competition effect inhibited drug molecules from permeating deeper into the bilayer. At high concentrations, borneol led to the formation of water pores and long-lived reversed micelles. This improved the permeation of osthole and possibly other hydrophobic or hydrophilic drugs through the SC. Our simulation results were supported by Franz diffusion tests and transmission electron microscope (TEM) experiments.
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