Document Detail


Effect of 1,4-cyclohexanediol on percutaneous absorption and penetration of azelaic acid.
MedLine Citation:
PMID:  20025951     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The objective of this study is to investigate the effect of 1,4-cyclohexanediol as a retardant on the percutaneous absorption and penetration of azelaic acid. Hairless rat skin was mounted on Franz diffusion cells and treated with topical formulations containing solubilized azelaic acid with and without 1,4-cyclohexanediol. The skin was separated into stratum corneum and the deeper skin layers. The azelaic acid collected in receptor medium and each layer at the end of each time point was extracted and quantified. A significant decrease in flux across the skin suggests a penetration retardation effect of 1,4-cyclohexanediol (42.50 microg/cm(2)/h in the presence of vs. 76.25 microg/cm(2)/h in the absence of) at active loading level of 1.13 mg/cm(2). The penetration retardation effect was also observed at higher active loading level (2.82 mg/cm(2)). Furthermore, presence of 1,4-cyclohexanediol in the topical formulation did not reduce the skin and epidermal retention of azelaic acid, suggesting its potential use in the development of superior topical formation for reducing potential systematic side effect while maintaining therapeutic efficiency.
Authors:
Nan Li; Qian Su; Fengping Tan; Jerry Zhang
Publication Detail:
Type:  In Vitro; Journal Article     Date:  2009-12-16
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  387     ISSN:  1873-3476     ISO Abbreviation:  Int J Pharm     Publication Date:  2010 Mar 
Date Detail:
Created Date:  2010-02-15     Completed Date:  2010-05-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  167-71     Citation Subset:  IM    
Copyright Information:
2009 Elsevier B.V. All rights reserved.
Affiliation:
Tianjin Key Laboratory of Drug Delivery & High-Efficiency, Department of Pharmaceutics, College of Pharmaceutical Science and Technology, Tianjin University, Tianjin, PR China.
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MeSH Terms
Descriptor/Qualifier:
Administration, Cutaneous
Animals
Cyclohexanols / chemistry*
Dermatologic Agents / administration & dosage,  adverse effects,  pharmacokinetics*
Dicarboxylic Acids / administration & dosage,  adverse effects,  pharmacokinetics*
Male
Permeability
Rats
Skin Absorption*
Chemical
Reg. No./Substance:
0/Cyclohexanols; 0/Dermatologic Agents; 0/Dicarboxylic Acids; 123-99-9/azelaic acid; 556-48-9/1,4-cyclohexanediol

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


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