Effects of Oxygen-Containing Terpenes as Skin Permeation Enhancers on the Lipoidal Pathways of Human Epidermal Membrane

The present study investigated the effects of oxygen-containing terpenes as skin permeation enhancers on the lipoidal pathways of human epidermal membrane (HEM). The enhancement (EHEM) effects of menthol, thymol, carvacrol, menthone, and cineole on the transport of a probe permeant, corticosterone,...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2009-10, Vol.98 (10), p.3617-3632
Main Authors: Chantasart, Doungdaw, Pongjanyakul, Thaned, Higuchi, William I., Li, S. Kevin
Format: Article
Language:English
Subjects:
Adult
Aged
Biological and medical sciences
Chromatography, Gas
Chromatography, High Pressure Liquid
Electric Impedance
Epidermis - chemistry
Epidermis - metabolism
Excipients
Female
General pharmacology
Heptanes - chemistry
Heptanes - pharmacology
human epidermal membrane
Humans
In Vitro Techniques
Lipids - chemistry
lipoidal pathway
Medical sciences
Middle Aged
Oils, Volatile - pharmacology
Oxygen - chemistry
oxygen-containing terpenes
Permeability
permeant
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Skin Absorption - drug effects
skin permeation enhancers
Solubility
Terpenes - chemistry
Terpenes - pharmacology
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Summary:The present study investigated the effects of oxygen-containing terpenes as skin permeation enhancers on the lipoidal pathways of human epidermal membrane (HEM). The enhancement (EHEM) effects of menthol, thymol, carvacrol, menthone, and cineole on the transport of a probe permeant, corticosterone, across HEM were determined. It was found that the enhancer potencies of menthol, thymol, carvacrol, and menthone were essentially the same and higher than that of cineole based on their aqueous concentration in the diffusion cell chamber at EHEM=4. Thymol and carvacrol also had the same EHEM=10 concentration further supporting that they had the same enhancer potency based on the aqueous concentration. The uptake amounts of terpene into the HEM stratum corneum (SC) intercellular lipid under the same conditions indicate that the intrinsic potencies of the studied terpenes are the same based on their concentration in the SC and similar to those of n-alkanol and n-alkylphenyl alcohol. Moreover, they are all better enhancers compared to branched-chain alkanol. The approximately same uptake enhancement of β-estradiol induced by the studied terpenes and alcohols at EHEM conditions into the SC intercellular lipids suggests that the mechanism of enhancement action for the terpenes and those of alcohols are essentially the same. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:3617–3632, 2009
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.21666