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Investigation of a Microemulsion Containing Clotrimazole and Itraconazole for Transdermal Delivery for the Treatment of Sporotrichosis.

Authors
  • Ferreira, Patricia G1
  • Noronha, Letícia1
  • Teixeira, Rafaela2
  • Vieira, Italo3
  • Borba-Santos, Luana P4
  • Viçosa, Alessandra5
  • de Moraes, Marcela6
  • Calil-Elias, Sabrina2
  • de Freitas, Zaida7
  • da Silva, Fernando C6
  • Rozental, Sônia4
  • Futuro, Débora O2
  • Ferreira, Vitor F8
  • 1 Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Niterói, RJ 24210-141, Brazil; Universidade Federal Fluminense, Faculdade de Farmácia, 24241-000 Niterói, RJ, Brazil. , (Brazil)
  • 2 Universidade Federal Fluminense, Faculdade de Farmácia, 24241-000 Niterói, RJ, Brazil. , (Brazil)
  • 3 Universidade do Estado do Rio de Janeiro, Instituto de Química, 20550-900 Rio de Janeiro, RJ, Brazil. , (Brazil)
  • 4 Universidade Federal do Rio de Janeiro, Instituto de Biofísica Carlos Filho, Laboratório de Biologia Celular de Fungos, 21941-902 Rio de Janeiro, RJ, Brazil. , (Brazil)
  • 5 Fundação Oswaldo Cruz (FIOCRUZ), Farmanguinhos, 21045-900 Rio de Janeiro, RJ, Brazil. , (Brazil)
  • 6 Departamento de Química Orgânica, Instituto de Química, Universidade Federal Fluminense, Niterói, RJ 24210-141, Brazil. , (Brazil)
  • 7 Universidade Federal do Rio de Janeiro, Farmácia Universitária, 21941-170 Rio de Janeiro, RJ, Brazil. , (Brazil)
  • 8 Universidade Federal Fluminense, Faculdade de Farmácia, 24241-000 Niterói, RJ, Brazil. Electronic address: [email protected] , (Brazil)
Type
Published Article
Journal
Journal of Pharmaceutical Sciences
Publisher
Elsevier
Publication Date
Oct 08, 2019
Identifiers
DOI: 10.1016/j.xphs.2019.10.009
PMID: 31604084
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

The aim of this study was to develop a microemulsion (ME) formulation containing an association of itraconazole (ITC) and clotrimazole (CLT) as a transdermal delivery system for the treatment of sporotrichosis. Pseudoternary phase diagrams were constructed to optimize the ME formulation. The ME formulation selected contained 1% (w/w) ITC and 1% (w/w) CLT and was composed of 23.07% Tween® 60 (surfactant), 23.07% propylene glycol (cosurfactant/cosolvent), 30.77% benzyl alcohol (oil), and 21.09% water. The ITC/CLT-loaded ME (ITC/CLT-ME) had a droplet size value of 217 ± 0.9 nm, with a polydispersity index of 0.5 ± 0.1. Permeation experiments on pig ear skin were conducted for ITC/CLT-ME, and the results indicated that the drug permeation performance was influenced by CLT, indicating that CLT acts as a promoter enhancer. In the in vitro antifungal activity assay using Sporothrix brasiliensis yeast, the inhibition halo produced by ITC/CLT-ME exhibited a mean diameter of 43.67 ± 2.31 mm. The ITC/CLT-ME formulation did not cause skin irritation in mice. The results suggest that ITC/CLT-ME is a promising tool for the transdermal treatment of sporotrichosis. Copyright © 2019 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

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