Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis
The production of ergosterol lipid involves the activity of different enzymes and is a crucial event for the Leishmania membrane homeostasis. Such enzymes can be blocked by azoles and allylamines drugs, such as the antifungal butenafine chloride. This drug was active on parasites that cause cutaneou...
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| Format: | Article |
| Language: | English |
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Wiley
2021-01-01
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| Series: | Journal of Immunology Research |
| Online Access: | http://dx.doi.org/10.1155/2021/8828750 |
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| author | Adriana Bezerra-Souza Jéssica A. Jesus Márcia D. Laurenti Aikaterini Lalatsa Dolores R. Serrano Luiz Felipe D. Passero |
| author_facet | Adriana Bezerra-Souza Jéssica A. Jesus Márcia D. Laurenti Aikaterini Lalatsa Dolores R. Serrano Luiz Felipe D. Passero |
| author_sort | Adriana Bezerra-Souza |
| collection | DOAJ |
| description | The production of ergosterol lipid involves the activity of different enzymes and is a crucial event for the Leishmania membrane homeostasis. Such enzymes can be blocked by azoles and allylamines drugs, such as the antifungal butenafine chloride. This drug was active on parasites that cause cutaneous and visceral leishmaniasis. Based on the leishmanicidal activity of butenafine chloride and considering the absence of reports about the therapeutic potential of this drug in cutaneous leishmaniasis, the present work is aimed at analyzing the efficacy of butenafine formulated in two different topical delivery systems, the self-nanoemulsifying drug delivery systems (BUT-SNEDDS) and in a SNEDDS-based nanogel (BUT-SNEDDS gel) as well as in the free form in experimental cutaneous leishmaniasis. Physical studies showed that both formulations were below 300 nm with low polydispersity (<0.5) and good colloidal stability (around -25 mV). Increased steady-state flux was reported for nanoenabled butenafine formulations with reduced lag time in Franz cell diffusion assays across Strat-M membranes. No toxic or inflammatory reactions were detected in animals treated with BUT-SNEDDS, BUT-SNEDDS gel, or butenafine. Animals topically treated with butenafine (free or nanoformulated) showed small dermal lesions and low tissue parasitism. Furthermore, BUT-SNEDD gel and butenafine presented similar efficacy than the standard drug Glucantime given by the intralesional route. Increased levels of IFN-γ were observed in animals treated with BUT-SNEDDS gel or butenafine. Based on these data, the antifungal drug butenafine chloride can be considered an interesting repurposed drug for the treatment of cutaneous leishmaniasis. |
| format | Article |
| id | doaj-art-3d3e3a8e6f334a4a802710179e6d8d4e |
| institution | Kabale University |
| issn | 2314-8861 2314-7156 |
| language | English |
| publishDate | 2021-01-01 |
| publisher | Wiley |
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| series | Journal of Immunology Research |
| spelling | doaj-art-3d3e3a8e6f334a4a802710179e6d8d4e2025-02-03T01:10:53ZengWileyJournal of Immunology Research2314-88612314-71562021-01-01202110.1155/2021/88287508828750Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous LeishmaniasisAdriana Bezerra-Souza0Jéssica A. Jesus1Márcia D. Laurenti2Aikaterini Lalatsa3Dolores R. Serrano4Luiz Felipe D. Passero5Laboratory of Pathology of Infectious Diseases (LIM-50), Medical School, University of São Paulo, Avenida Dr. Arnaldo 455, 01246903 Cerqueira César, SP, BrazilLaboratory of Pathology of Infectious Diseases (LIM-50), Medical School, University of São Paulo, Avenida Dr. Arnaldo 455, 01246903 Cerqueira César, SP, BrazilLaboratory of Pathology of Infectious Diseases (LIM-50), Medical School, University of São Paulo, Avenida Dr. Arnaldo 455, 01246903 Cerqueira César, SP, BrazilBiomaterials, Bio-engineering and Nanomedicines (BioN) Laboratory, Institute of Biomedical and Biomolecular Sciences, School of Pharmacy and Biomedical Sciences, University of Portsmouth, White Swan Road, Portsmouth PO1 2DT, UKDepartment of Pharmaceutics and Food Technology and Instituto Universitario de Farmacia Industrial (IUFI), School of Pharmacy, Complutense University, Avenida Complutense, 28040 Madrid, SpainInstitute of Biosciences, São Paulo State University (UNESP), São Vicente, Praça Infante Dom Henrique, s/n, 11330-900 São Vicente, SP, BrazilThe production of ergosterol lipid involves the activity of different enzymes and is a crucial event for the Leishmania membrane homeostasis. Such enzymes can be blocked by azoles and allylamines drugs, such as the antifungal butenafine chloride. This drug was active on parasites that cause cutaneous and visceral leishmaniasis. Based on the leishmanicidal activity of butenafine chloride and considering the absence of reports about the therapeutic potential of this drug in cutaneous leishmaniasis, the present work is aimed at analyzing the efficacy of butenafine formulated in two different topical delivery systems, the self-nanoemulsifying drug delivery systems (BUT-SNEDDS) and in a SNEDDS-based nanogel (BUT-SNEDDS gel) as well as in the free form in experimental cutaneous leishmaniasis. Physical studies showed that both formulations were below 300 nm with low polydispersity (<0.5) and good colloidal stability (around -25 mV). Increased steady-state flux was reported for nanoenabled butenafine formulations with reduced lag time in Franz cell diffusion assays across Strat-M membranes. No toxic or inflammatory reactions were detected in animals treated with BUT-SNEDDS, BUT-SNEDDS gel, or butenafine. Animals topically treated with butenafine (free or nanoformulated) showed small dermal lesions and low tissue parasitism. Furthermore, BUT-SNEDD gel and butenafine presented similar efficacy than the standard drug Glucantime given by the intralesional route. Increased levels of IFN-γ were observed in animals treated with BUT-SNEDDS gel or butenafine. Based on these data, the antifungal drug butenafine chloride can be considered an interesting repurposed drug for the treatment of cutaneous leishmaniasis.http://dx.doi.org/10.1155/2021/8828750 |
| spellingShingle | Adriana Bezerra-Souza Jéssica A. Jesus Márcia D. Laurenti Aikaterini Lalatsa Dolores R. Serrano Luiz Felipe D. Passero Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis Journal of Immunology Research |
| title | Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis |
| title_full | Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis |
| title_fullStr | Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis |
| title_full_unstemmed | Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis |
| title_short | Nanoemulsified Butenafine for Enhanced Performance against Experimental Cutaneous Leishmaniasis |
| title_sort | nanoemulsified butenafine for enhanced performance against experimental cutaneous leishmaniasis |
| url | http://dx.doi.org/10.1155/2021/8828750 |
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