Titre
Simultaneous Delivery of Econazole, Terbinafine and Amorolfine with Improved Cutaneous Bioavailability: A Novel Micelle-Based Antifungal "Tri-Therapy".
Type
article
Institution
UNIL/CHUV/Unisanté + institutions partenaires
Périodique
Auteur(s)
Gou, S.
Auteure/Auteur
Monod, M.
Auteure/Auteur
Salomon, D.
Auteure/Auteur
Kalia, Y.N.
Auteure/Auteur
Liens vers les personnes
Liens vers les unités
ISSN
1999-4923
Statut éditorial
Publié
Date de publication
2022-01-24
Volume
14
Numéro
2
Première page
271
Peer-reviewed
Oui
Langue
anglais
Notes
Publication types: Journal Article
Publication Status: epublish
Publication Status: epublish
Résumé
Lack of accurate diagnosis and the use of formulations designed to address the poor aqueous solubility of antifungal agents, but not optimized for delivery, contribute to unsatisfactory outcomes for topical treatment of cutaneous mycoses. The objective of this study was to develop a micelle-based antifungal formulation containing econazole (ECZ), terbinafine (TBF) and amorolfine (AMF) using D-α-tocopheryl polyethylene glycol succinate (TPGS) for simultaneous cutaneous delivery of three agents with complementary mechanisms of action. The antifungal "tri-therapy" micelle-based formulation containing 0.1% ECZ, 0.1% TBF and 0.025% AMF had a drug loading 10-fold lower than the "reference" marketed formulations (Pevaryl <sup>®</sup> , 1% ECZ; Lamisil <sup>®</sup> , 1% TBF; Loceryl <sup>®</sup> , 0.25% AMF). Finite dose application of the micelle-based formulation for 6 h resulted in a statistically equivalent deposition of ECZ (p > 0.05) and TBF (p > 0.05) from the 2 systems, and a 2-fold higher accumulation of AMF (p = 0.017). Antifungal concentrations above MIC <sub>80</sub> against Trichophyton rubrum were achieved in each skin layer with the "tri-therapy", which also exhibited a preferential deposition of each antifungal agent in pilosebaceous unit (PSU)-containing biopsies as compared with PSU-free biopsies (p < 0.05). A planned clinical study will test whether these promising results translate to improved therapeutic outcomes in vivo.
PID Serval
serval:BIB_85B3563E1E19
PMID
Open Access
Oui
Date de création
2022-03-07T10:41:11.460Z
Date de création dans IRIS
2025-05-21T02:06:11Z
Fichier(s)![Vignette d'image]()
En cours de chargement...
Nom
35214004_BIB_85B3563E1E19.pdf
Version du manuscrit
published
Licence
https://creativecommons.org/licenses/by/4.0
Taille
2.68 MB
Format
Adobe PDF
PID Serval
serval:BIB_85B3563E1E19.P001
URN
urn:nbn:ch:serval-BIB_85B3563E1E194
Somme de contrôle
(MD5):9569178c23455d7d5e2d795516844edb