Document Detail


In vivo quantification of acyclovir exposure in the dermis following iontophoresis of semisolid formulations.
MedLine Citation:
PMID:  18623192     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The objective was to quantify acyclovir (ACV) exposure in the dermis following iontophoresis of nontraditional (pH-11 gels) and traditional (neutral cream) topical formulations of ACV. Given that the application time of a formulation on the skin can be significantly reduced with iontophoresis, the use of formulations optimized for iontophoretic delivery was explored to maximize the delivery of ACV to the site of action for the treatment of Herpes-labialis. Microdialysis probes were inserted into the shaved skin of tranquilized rabbits. Iontophoresis was performed at a constant current density of 200 microA/cm(2) for 60 min using a single-use drug cartridge filled with the following formulations: neutral cream, soluble fraction of the same cream (anodal and cathodal-current), or two formulations of pH-11 gels, one without and one with stabilizers and preservatives (cathodal-current). Results showed that only the ACV in the water phase of the cream is available for transport. All of the pH-11 gels exhibited a statistically significant (p < 0.001) increase in ACV dermis exposure compared to the neutral cream formulations without any additional sign of skin irritation. In conclusion, iontophoresis of ACV pH-11 gels provides higher ACV concentrations in the dermis than iontophoresis of neutral cream formulations, which could result in a better clinical outcome.
Authors:
Chinmay Shukla; Phillip Friden; Ravi Juluru; Grazia Stagni
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  98     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2009 Mar 
Date Detail:
Created Date:  2009-02-03     Completed Date:  2009-04-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  917-25     Citation Subset:  IM    
Copyright Information:
(c) 2008 Wiley-Liss, Inc. and the American Pharmacists Association
Affiliation:
Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, 75 DeKalb Ave., Brooklyn, New York 11201, USA.
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MeSH Terms
Descriptor/Qualifier:
Acyclovir / administration & dosage*,  pharmacokinetics
Animals
Antiviral Agents / administration & dosage*,  pharmacokinetics
Female
Hydrogen-Ion Concentration
Iontophoresis / methods
Microdialysis
Ointments / administration & dosage*,  chemistry*,  pharmacokinetics
Rabbits
Skin / metabolism*
Chemical
Reg. No./Substance:
0/Antiviral Agents; 0/Ointments; 59277-89-3/Acyclovir

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


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