Document Detail


Evaluation of skin permeation of β-blockers for topical drug delivery.
MedLine Citation:
PMID:  23208385     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: β-Blockers have recently become the main form of treatment of infantile hemangiomas. Due to the potential systemic adverse effects of β-blockers, topical skin treatment of the drugs is preferred. However, the effect and mechanism of dosage form pH upon skin permeation of these weak bases is not well understood. To develop an effective topical skin delivery system for the β-blockers, the present study evaluated skin permeation of β-blockers propranolol, betaxolol, timolol, and atenolol.
METHODS: Experiments were performed in side-by-side diffusion cells with human epidermal membrane (HEM) in vitro to determine the effect of donor solution pH upon the permeation of the β-blockers across HEM.
RESULTS: The apparent permeability coefficients of HEM for the β-blockers increased with their lipophilicity, suggesting the HEM lipoidal pathway as the main permeation mechanism of the β-blockers. The pH in the donor solution was a major factor influencing HEM permeation for the β-blockers with a 2- to 4-fold increase in the permeability coefficient per pH unit increase. This permeability versus pH relationship was found to deviate from theoretical predictions, possibly due to the effective stratum corneum pH being different from the pH in the donor solution.
CONCLUSIONS: The present results suggest the possibility of topical treatment of hemangioma using β-blockers.
Authors:
Doungdaw Chantasart; Jinsong Hao; S Kevin Li
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2012-12-04
Journal Detail:
Title:  Pharmaceutical research     Volume:  30     ISSN:  1573-904X     ISO Abbreviation:  Pharm. Res.     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-20     Completed Date:  2013-08-01     Revised Date:  2014-03-07    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  866-77     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Administration, Topical
Adrenergic beta-Antagonists / chemistry,  pharmacokinetics*
Adult
Atenolol / chemistry,  pharmacokinetics*
Betaxolol / chemistry,  pharmacokinetics*
Epidermis / metabolism
Humans
Middle Aged
Propranolol / chemistry,  pharmacokinetics*
Skin / metabolism*
Skin Absorption
Timolol / chemistry,  pharmacokinetics*
Young Adult
Grant Support
ID/Acronym/Agency:
GM063559/GM/NIGMS NIH HHS; R01 GM063559/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 50VV3VW0TI/Atenolol; 817W3C6175/Timolol; 9Y8NXQ24VQ/Propranolol; O0ZR1R6RZ2/Betaxolol
Comments/Corrections

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


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