Document Detail


Enhanced iontophoretic delivery of buspirone hydrochloride across human skin using chemical enhancers.
MedLine Citation:
PMID:  12972337     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Buspirone hydrochloride (BH) is a structurally and pharmacologically unique anxiolytic that is used to treat a variety of different anxiety conditions. The marketed product is named BuSpar. The in vitro iontophoretic delivery of BH through human skin was investigated in order to evaluate the feasibility of delivering a therapeutic dose of BH by this route. We also examined the influence of co-formulations of chemical enhancers (Azone, oleic acid, menthone, cineole, and terpineol) on BH permeation, both without iontophoresis and with iontophoresis-to look for possible synergistic effects. By applying iontophoresis at 0.5 mA/cm(2), it was possible to achieve a BH steady state flux of approximately 350 microg/cm(2)h, which would be therapeutically effective if clinically duplicated. Importantly, 24 h of iontophoresis at 0.5 mA/cm(2) did not affect skin morphology and after the current was switched off, the skin's permeability to BH rapidly reverted to its pre-iontophoretic level. Without iontophoreis, BH transdermal flux was significantly enhanced by the application of 2.5% (v/v) concentrations of Azone, oleic acid, or menthone but not cineole or terpineol. Furthermore, this paper identified a synergistic transport enhancement effect developing when very low current (0.025 mA/cm(2)) iontophoresis was applied in conjunction with Azone treatment.
Authors:
Victor M Meidan; Mohammad Al-Khalili; Bozena B Michniak
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  264     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2003 Oct 
Date Detail:
Created Date:  2003-09-15     Completed Date:  2004-02-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  73-83     Citation Subset:  IM    
Affiliation:
Department of Physiology and Pharmacology, University of Medicine and Dentistry of New Jersey, Newark, NJ 07103, USA.
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MeSH Terms
Descriptor/Qualifier:
Adjuvants, Pharmaceutic / pharmacology*
Administration, Cutaneous
Anti-Anxiety Agents / administration & dosage,  chemistry,  pharmacokinetics*
Azepines / pharmacology
Buspirone / administration & dosage,  chemistry,  pharmacokinetics*
Chemistry, Pharmaceutical
Chromatography, High Pressure Liquid
Cyclohexanols / pharmacology
Cyclohexenes
Humans
Iontophoresis
Menthol / pharmacology
Monoterpenes / pharmacology
Oleic Acid / pharmacology
Skin / drug effects*,  metabolism,  ultrastructure
Skin Absorption / drug effects*
Time Factors
Chemical
Reg. No./Substance:
0/Adjuvants, Pharmaceutic; 0/Anti-Anxiety Agents; 0/Azepines; 0/Cyclohexanols; 0/Cyclohexenes; 0/Monoterpenes; 112-80-1/Oleic Acid; 1490-04-6/Menthol; 36505-84-7/Buspirone; 470-82-6/cineole; 59227-89-3/laurocapram; 89-80-5/menthone; 98-55-5/alpha-terpineol

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


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