title: Econazole imprinted textiles with antifungal activity.
abstract: In this work, we propose pharmaceutical textiles imprinted with lipid microparticles of Econazole nitrate (ECN) as a mean to improve patient compliance while maintaining drug activity. Lipid microparticles were prepared and characterized by laser diffraction (3.5±0.1 μm). Using an optimized screen-printing method, microparticles were deposited on textiles, as observed by scanning electron microscopy. The drug content of textiles (97±3 μg/cm(2)) was reproducible and stable up to 4 months storage at 25 °C/65% Relative Humidity. Imprinted textiles exhibited a thermosensitive behavior, as witnessed by a fusion temperature of 34.8 °C, which enabled a larger drug release at 32 °C (temperature of the skin) than at room temperature. In vitro antifungal activity of ECN textiles was compared to commercial 1% (wt/wt) ECN cream Pevaryl®. ECN textiles maintained their antifungal activity against a broad range of Candida species as well as major dermatophyte species. In vivo, ECN textiles also preserved the antifungal efficacy of ECN on cutaneous candidiasis infection in mice. Ex vivo percutaneous absorption studies demonstrated that ECN released from pharmaceutical textiles concentrated more in the upper skin layers, where the fungal infections develop, as compared to dermal absorption of Pevaryl®. Overall, these results showed that this technology is promising to develop pharmaceutical garments textiles for the treatment of superficial fungal infections.
authors.affiliation: Faculty of Pharmacy, Université de Montréal, PO Box 6128, Station Centre-Ville, Montreal, QC H3C 3J7, Canada.
authors.forename: Mirza Akram
authors.initials: MA
authors.lastname: Hossain
authors.affiliation: Faculty of Pharmacy, Université de Montréal, PO Box 6128, Station Centre-Ville, Montreal, QC H3C 3J7, Canada.
authors.forename: Augustine
authors.initials: A
authors.lastname: Lalloz
authors.affiliation: Biomod Concepts Inc, Sainte-Julie, QC J3E 1Y6, Canada.
authors.forename: Aicha
authors.initials: A
authors.lastname: Benhaddou
authors.affiliation: Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, EA1155 - IICiMed, UFR de Sciences Pharmaceutiques et Biologiques, Faculté de pharmacie, Nantes Atlantique Universités, Nantes, France; Laboratoire de Parasitologie-Mycologie, Institut de Biologie, CHU de Nantes, Nantes, France.
authors.forename: Fabrice
authors.initials: F
authors.lastname: Pagniez
authors.affiliation: Institute for Research in Immunology and Cancer and Department of Biochemistry and Molecular Medicine, Université de Montréal, Montreal, QC H3C 3J7, Canada.
authors.forename: Martine
authors.initials: M
authors.lastname: Raymond
authors.affiliation: Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, EA1155 - IICiMed, UFR de Sciences Pharmaceutiques et Biologiques, Faculté de pharmacie, Nantes Atlantique Universités, Nantes, France; Laboratoire de Parasitologie-Mycologie, Institut de Biologie, CHU de Nantes, Nantes, France.
authors.forename: Patrice
authors.initials: P
authors.lastname: Le Pape
authors.affiliation: Biomod Concepts Inc, Sainte-Julie, QC J3E 1Y6, Canada.
authors.forename: Pierre
authors.initials: P
authors.lastname: Simard
authors.affiliation: Biomod Concepts Inc, Sainte-Julie, QC J3E 1Y6, Canada.
authors.forename: Karine
authors.initials: K
authors.lastname: Théberge
authors.affiliation: Faculty of Pharmacy, Université de Montréal, PO Box 6128, Station Centre-Ville, Montreal, QC H3C 3J7, Canada. Electronic address: Jeanne.leblond-chain@umontreal.ca.
authors.forename: Jeanne
authors.initials: J
authors.lastname: Leblond
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D002177:Candidiasis / Q000188:drug therapy; D004337:Drug Carriers / Q000737:chemistry; D004464:Econazole / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D008055:Lipids / Q000737:chemistry; D051379:Mice; D054802:Molecular Imprinting / Q000379:methods; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013552:Swine; D013696:Temperature; D013784:Textiles
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D008055:Lipids; D004464:Econazole
keywords: Candida; Econazole nitrate; Fungal infection; Lipid microparticles; Thermo-responsive formulation; Topical administration