Investigation of pH Influence on Skin Permeation Behavior of Weak Acids Using Nonsteroidal Anti-Inflammatory Drugs

Investigation of pH Influence on Skin Permeation Behavior of Weak Acids Using Nonsteroidal Anti-Inflammatory Drugs

As a continuing effort to understand the skin permeation behavior of weak acids and bases, the objectives of the present study were to evaluate skin permeation of nonsteroidal anti-inflammatory drugs (NSAIDs) under the influence of pH, investigate the mechanism of pH effect, and examine a previous h...

Full description

Saved in:
Bibliographic Details
Published in:Journal of pharmaceutical sciences Vol. 104; no. 10; p. 3459
Main Authors: Chantasart, Doungdaw, Chootanasoontorn, Siriwan, Suksiriworapong, Jiraphong, Li, S Kevin
Format: Journal Article
Language:English
Published: United States 01-10-2015
Subjects:
Acids - chemistry
Acids - pharmacokinetics
Administration, Cutaneous
Adult
Algorithms
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Chromatography, High Pressure Liquid
Electric Impedance
Female
Humans
Hydrogen-Ion Concentration
In Vitro Techniques
Lipids - chemistry
Middle Aged
Models, Theoretical
Permeability
Skin Absorption
nonsteroidal anti-inflammatory drugs
stratum corneum
topical
transdermal
permeability
drug transport
pH
skin
Online Access:Get more information
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:As a continuing effort to understand the skin permeation behavior of weak acids and bases, the objectives of the present study were to evaluate skin permeation of nonsteroidal anti-inflammatory drugs (NSAIDs) under the influence of pH, investigate the mechanism of pH effect, and examine a previous hypothesis that the effective skin pH for drug permeation is different from donor solution pH. In vitro permeability experiments were performed in side-by-side diffusion cells with diclofenac, ibuprofen, flurbiprofen, ketoprofen, and naproxen and human skin. The donor solution pH significantly affected skin permeation of NSAIDs, whereas no effect of the receiver pH was observed. Similar to previous observations, the apparent permeability coefficient versus donor solution pH relationships deviated from the predictions (fractions of unionized NSAIDs) according to the acid/base theory. The influences of the viable epidermis barrier, polar pathway transport, ion permeation across skin, and effective skin pH were investigated. The effective pH values for skin permeation determined using the NSAIDs (weak acids) in this study were different from those obtained previously with a weak base at the same donor solution pH conditions, suggesting that the observed permeability-pH relationships could not be explained solely by possible pH differences between skin and donor solution.
ISSN:1520-6017
DOI:10.1002/jps.24556