title: Antifungal activity of topical microemulsion containing a thiophene derivative.
abstract: Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 μg . mL(-1)) and good activity against C. neoformans (MIC = 17 μg . mL(-1)). Candida species were susceptible to ME-5CN05 (70-140 μg . mL(-1)), but C. neoformans was much more, presenting a MIC value of 2.2 μg . mL(-1). The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas Universidade Estadual da Paraíba Campina GrandePB Brazil Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil.
authors.forename: Geovani Pereira
authors.initials: GP
authors.lastname: Guimarães
authors.affiliation: Departmento de Farmácia Universidade Estadual da Paraíba Campina GrandePB Brazil Departmento de Farmácia, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil.
authors.forename: Mysrayn Yargo
authors.initials: MY
authors.lastname: de Freitas Araújo Reis
authors.affiliation: Departmento de Farmácia Universidade Estadual da Paraíba Campina GrandePB Brazil Departmento de Farmácia, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil.
authors.forename: Dayanne Tomaz Casimiro
authors.initials: DT
authors.lastname: da Silva
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas Universidade Estadual da Paraíba Campina GrandePB Brazil Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil. ; Laboratório de Síntese e Vetorização de Moléculas Departamento de Ciências Biológicas Universidade Estadual da Paraíba João PessoaPB Brazil Laboratório de Síntese e Vetorização de Moléculas, Departamento de Ciências Biológicas, Universidade Estadual da Paraíba, João Pessoa, PB, Brazil.
authors.forename: Francisco Jaime Bezerra Mendonça
authors.initials: FJ
authors.lastname: Junior
authors.affiliation: Department of Civil, Chemical and Environmental Engineering, Chemical Engineering Pole Genoa University Genova Italy Department of Civil, Chemical and Environmental Engineering, Chemical Engineering Pole, Genoa University, Genova, Italy.
authors.forename: Attílio
authors.initials: A
authors.lastname: Converti
authors.affiliation: Departmento de Tecnologia Bioquímico-Farmacêutica Universidade de São Paulo São PauloSP Brazil Departmento de Tecnologia Bioquímico-Farmacêutica, Universidade de São Paulo, São Paulo, SP, Brazil.
authors.forename: Adalberto
authors.initials: A
authors.lastname: Pessoa
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas Universidade Estadual da Paraíba Campina GrandePB Brazil Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil. ; Departmento de Farmácia Universidade Estadual da Paraíba Campina GrandePB Brazil Departmento de Farmácia, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil.
authors.forename: Bolívar Ponciano Goulart
authors.initials: BP
authors.lastname: de Lima Damasceno
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas Universidade Estadual da Paraíba Campina GrandePB Brazil Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil. ; Departmento de Farmácia Universidade Estadual da Paraíba Campina GrandePB Brazil Departmento de Farmácia, Universidade Estadual da Paraíba, Campina Grande, PB, Brazil.
authors.forename: José Alexsandro
authors.initials: JA
authors.lastname: da Silva
mesh_terms: D000891:Anti-Infective Agents, Local / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D003455:Cryptococcus neoformans / Q000187:drug effects*; D004655:Emulsions / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D013876:Thiophenes / Q000494:pharmacology*
chemical_list: D000891:Anti-Infective Agents, Local; D000935:Antifungal Agents; D004655:Emulsions; D013876:Thiophenes
keywords: Cryptococcus neoformans; antifungal susceptibility; microemulsion; thiophene derivatives