Document Detail


Effect of physicochemical properties of cyclic terpenes on their ex vivo skin absorption and elimination kinetics.
MedLine Citation:
PMID:  16260121     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: The terpenes disturb lipid arrangement in the intercellular region of the stratum corneum (SC) that leads to the increased permeability of the skin. This effect is used in technology of transdermal drug forms and depends on physicochemical properties of terpenes and their amounts penetrated to the stratum corneum; however terpenes do not need penetrate into viable skin tissue and this event is not even desired. OBJECTIVE: To correlate skin absorption and elimination kinetics of four cyclic terpenes, namely alpha-pinene, beta-pinene, eucalyptol and terpinen-4-ol, applied as neat substance with their physicochemical properties. METHODS: The terpenes were applied onto the human skin in vitro, and after 1-4 h their content in the separated by a tape-stripping method stratum corneum layers and in the epidermis/dermis was determined using GC. Similarly, the amounts of terpenes in the skin were analysed during 4 h following 1 h absorption. RESULTS: The fastest and progressive penetration into all skin layers was observed for terpinen-4-ol. All studied terpenes are absorbed in the viable epidermis/dermis, however penetration into this layers is time-dependent process, constantly increasing during 4 h. Like for stratum corneum, the largest cumulation in epidermis/dermis was observed for terpinen-4-ol. The elimination of terpenes from the stratum corneum was fast, especially in deeper layers, and much faster if the initial cumulation was small. CONCLUSION: Investigated cyclic terpenes represent different penetration and elimination characteristics and do not permeate across the skin to the acceptor medium due to large cumulation in the skin tissue. The penetration of terpenes into stratum corneum is greater if their log P-value is close to 3.
Authors:
Krzysztof Cal; Katarzyna Kupiec; Malgorzata Sznitowska
Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't     Date:  2005-11-02
Journal Detail:
Title:  Journal of dermatological science     Volume:  41     ISSN:  0923-1811     ISO Abbreviation:  J. Dermatol. Sci.     Publication Date:  2006 Feb 
Date Detail:
Created Date:  2006-01-18     Completed Date:  2006-03-16     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9011485     Medline TA:  J Dermatol Sci     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  137-42     Citation Subset:  IM    
Affiliation:
Medical University of Gdansk, Department of Pharmaceutical Technology, Hallera 107, 80-416 Gdansk, Poland. kcal@wp.pl
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MeSH Terms
Descriptor/Qualifier:
Adult
Bicyclo Compounds / pharmacokinetics,  pharmacology
Cell Membrane Permeability
Chemistry, Physical
Cyclohexanols / pharmacokinetics,  pharmacology
Dermis / metabolism
Diffusion
Epidermis / metabolism
Female
Humans
Kinetics
Middle Aged
Monoterpenes / pharmacokinetics,  pharmacology
Physicochemical Phenomena
Skin Absorption*
Terpenes / pharmacokinetics*,  pharmacology*
Chemical
Reg. No./Substance:
0/Bicyclo Compounds; 0/Cyclohexanols; 0/Monoterpenes; 0/Terpenes; 127-91-3/beta-pinene; 470-82-6/cineole; 562-74-3/terpinenol-4; 80-56-8/alpha-pinene

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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