title: Influence of penetration enhancers and molecular weight in antifungals permeation through bovine hoof membranes and prediction of efficacy in human nails.
abstract: 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.
authors.affiliation: Pharmaceutical Quality Control Laboratory, School of Pharmacy, UFRGS, Av. Ipiranga, 2752 Lab. 402, Bairro Santana, CEP 90610-000, Porto Alegre, RS, Brazil. Electronic address: diogomiron@outlook.com.
authors.forename: D
authors.initials: D
authors.lastname: Miron
authors.forename: R
authors.initials: R
authors.lastname: Cornelio
authors.forename: J
authors.initials: J
authors.lastname: Troleis
authors.forename: J
authors.initials: J
authors.lastname: Mariath
authors.forename: A R
authors.initials: AR
authors.lastname: Zimmer
authors.forename: P
authors.initials: P
authors.lastname: Mayorga
authors.forename: E E S
authors.initials: EE
authors.lastname: Schapoval
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000378:metabolism*; D001205:Ascorbic Acid / Q000737:chemistry; D002417:Cattle; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D006724:Hoof and Claw / Q000378:metabolism*; D006801:Humans; D008970:Molecular Weight; D009262:Nails / Q000378:metabolism*; D010539:Permeability / Q000187:drug effects*
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D001205:Ascorbic Acid
keywords: Acetylcysteine; Ascorbic acid; Butenafine; Butenafine hydrochloride; Fluconazole; Geraniol; Miconazole; Nerol; Terbinafine; Terbinafine hydrochloride