title: Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis.
abstract: Cutaneous leishmaniasis (CL) is a resistant form of leishmaniasis that is caused by a parasite belonging to the genus Leishmania. FLU-loaded microemulsions (MEs) were developed by phase diagram for topical administration of fluconazole (FLU) as prominent alternative to combat CL. Three MEs called F1, F2, and F3 (F1-60% 50 M phosphate buffer at pH 7.4 (PB) as aqueous phase, 10% cholesterol (CHO) as oil phase, and 30% soy phosphatidylcholine/oil polyoxyl-60 hydrogenated castor oil/sodium oleate (3/8/6) (S) as surfactant; F2-50% PB, 10% CHO, and 40% S; F3-40% PB, 10% CHO, and 50 % S) were characterized by droplet size analysis, zeta potential analysis, X-ray diffraction, continuous flow, texture profile analysis, and in vitro bioadhesion. MEs presented pseudoplastic flow and thixotropy was dependent on surfactant concentration. Droplet size was not affected by FLU. FLU-loaded MEs improved the FLU safety profile that was evaluated using red cell haemolysis and in vitro cytotoxicity assays with J-774 mouse macrophages. FLU-unloaded MEs did not exhibit leishmanicidal activity that was performed using MTT colourimetric assays; however, FLU-loaded MEs exhibited activity. Therefore, these MEs have potential to modulate FLU action, being a promising platform for drug delivery systems to treat CL.
authors: Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil.
authors: Marcela Brito
authors: 0000-0002-1616-2122
authors: MB
authors: Oliveira
authors: Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil.
authors: Giovana
authors: 0000-0003-1041-5835
authors: G
authors: Calixto
authors: Department of Clinical Analysis, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil.
authors: Márcia
authors: M
authors: Graminha
authors: Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, 11400 Montevideo, Uruguay.
authors: Hugo
authors: H
authors: Cerecetto
authors: Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, 11400 Montevideo, Uruguay.
authors: Mercedes
authors: M
authors: González
authors: Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil.
authors: Marlus
authors: 0000-0002-6698-0545
authors: M
authors: Chorilli
mesh_terms: D000268:Adhesiveness / Q000187:drug effects; D000287:Administration, Topical; D000818:Animals; D002460:Cell Line; D004655:Emulsions / Q000737:chemistry*; D005260:Female; D015725:Fluconazole / Q000008:administration & dosage* / Q000494:pharmacology / Q000627:therapeutic use*; D006244:Hardness; D006801:Humans; D066298:In Vitro Techniques; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy*; D008807:Mice, Inbred BALB C; D010316:Particle Size; D044367:Phase Transition / Q000187:drug effects; D012212:Rheology / Q000187:drug effects; D055672:Static Electricity; D034421:Sus scrofa; D014961:X-Ray Diffraction
chemical_list: D004655:Emulsions; D015725:Fluconazole
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