Influence of penetration enhancers and molecular weight in antifungals permeation through bovine hoof membranes and prediction of efficacy in human nails

This work aimed to evaluate the effect of different substances on the permeation of geraniol through bovine hoof membranes. Different penetration enhancers were able to increase the permeability up to 25 times compared to control. It was demonstrated that acetilcysteine in association with ascorbic...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmaceutical sciences 2014-01, Vol.51, p.20-25
Main Authors: Miron, D., Cornelio, R., Troleis, J., Mariath, J., Zimmer, A.R., Mayorga, P., Schapoval, E.E.S.
Format: Article
Language:English
Subjects:
Animals
Antifungal Agents - metabolism
Ascorbic Acid - chemistry
Butenafine
Cattle
Chemistry, Pharmaceutical - methods
Drug Carriers - chemistry
Fluconazole
Geraniol
Hoof and Claw - metabolism
Humans
Miconazole
Molecular Weight
Nails - metabolism
Nerol
Permeability - drug effects
Terbinafine
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:This work aimed to evaluate the effect of different substances on the permeation of geraniol through bovine hoof membranes. Different penetration enhancers were able to increase the permeability up to 25 times compared to control. It was demonstrated that acetilcysteine in association with ascorbic acid increased the permeation, even in acid formulations. In addition, some antifungal drugs were incorporated into a gel formulation of HPMC containing acetylcysteine 5% and ascorbic acid 0.2% and then the permeation coefficient through bovine hoof membranes was evaluated. The relationship between permeability and molecular weight was established for fluconazole, miconazole, terbinafine, butenafine, geraniol and nerol. Geraniol and nerol, the antifungals with lower molecular weight, had the better permeability results. Permeability coefficients for nail plates were estimated and geraniol demonstrated similar or even better efficacy index values against T. rubrum, T. menthagrophytes and M. canis compared with terbinafine and miconazole.
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2013.08.032