| 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 |
Related Documents
:
|
12524177 - Retinoic acid involvement in the reciprocal neurotrophic interactions between newt spin... 23411307 - Fatty acid composition of cooked chicken meat and chicken meat products as influenced b... 11509747 - Embryonic subcellular distribution of 13-cis- and all-trans-retinoic acid indicates dif... 19573917 - Nb4 cells treated with all-trans retinoic acid generate toxic reactive oxygen species t... 832337 - Effects of alpha-tocopherol analogs on lysosome membranes and fatty acid monolayers. 22457707 - Correction: identification of amino acid propensities that are strong determinants of l... |
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. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| 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
Previous Document: Long-term stabilization of recombinant human interferon alpha 2b in aqueous solution without serum a...
Next Document: Properties of enteric coated sodium valproate pellets.