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BioMed Research International
Volume 2015, Article ID 396894, 12 pages
http://dx.doi.org/10.1155/2015/396894
Research Article

Development, Characterization, and In Vitro Biological Performance of Fluconazole-Loaded Microemulsions for the Topical Treatment of Cutaneous Leishmaniasis

1Department of Drugs and Medicines, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil
2Department of Clinical Analysis, School of Pharmaceutical Sciences, UNESP, Rodovia Araraquara-Jaú, km. 1, Campus, 14801-902 Araraquara, SP, Brazil
3Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, 11400 Montevideo, Uruguay

Received 7 September 2014; Revised 18 December 2014; Accepted 20 December 2014

Academic Editor: Sami M. Nazzal

Copyright © 2015 Marcela Brito Oliveira et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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.