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Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment

Leishmaniasis is a disease caused by protozoa species of the Leishmania genus, and the current treatments face several difficulties and obstacles. Most anti-leishmanial drugs are administered intravenously, showing many side effects and drug resistance. The discovery of new anti-leishmanial compound...

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Autores principales: de Oliveira, Mariana Carla, Balbinot, Rodolfo Bento, Villa Nova, Mônica, Gonçalves, Renato Sonchini, Bidóia, Danielle Lazarin, Caetano, Wilker, Nakamura, Celso Vataru, Bruschi, Marcos Luciano
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10459651/
https://www.ncbi.nlm.nih.gov/pubmed/37631341
http://dx.doi.org/10.3390/pharmaceutics15082127
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author de Oliveira, Mariana Carla
Balbinot, Rodolfo Bento
Villa Nova, Mônica
Gonçalves, Renato Sonchini
Bidóia, Danielle Lazarin
Caetano, Wilker
Nakamura, Celso Vataru
Bruschi, Marcos Luciano
author_facet de Oliveira, Mariana Carla
Balbinot, Rodolfo Bento
Villa Nova, Mônica
Gonçalves, Renato Sonchini
Bidóia, Danielle Lazarin
Caetano, Wilker
Nakamura, Celso Vataru
Bruschi, Marcos Luciano
author_sort de Oliveira, Mariana Carla
collection PubMed
description Leishmaniasis is a disease caused by protozoa species of the Leishmania genus, and the current treatments face several difficulties and obstacles. Most anti-leishmanial drugs are administered intravenously, showing many side effects and drug resistance. The discovery of new anti-leishmanial compounds and the development of new pharmaceutical systems for more efficient and safer treatments are necessary. Copaiba oil-resin (CO) has been shown to be a promising natural compound against leishmaniasis. However, CO displays poor aqueous solubility and bioavailability. Self-emulsifying drug delivery systems (SEDDS) can provide platforms for release of hydrophobic compounds in the gastrointestinal tract, improving their aqueous solubilization, absorption and bioavailability. Therefore, the present work aimed to develop SEDDS containing CO and Soluplus(®) surfactant for the oral treatment of leishmaniasis. The design of the systems was accomplished using ternary phase diagrams. Emulsification and dispersion time tests were used to investigate the emulsification process in gastric and intestinal environments. The formulations were nanostructured and improved the CO solubilization. Their in vitro antiproliferative activity against promastigote forms of L. amazonensis and L. infantum, and low in vitro cytotoxicity against macrophages were also observed. More studies are necessary to determine effectiveness of SOL in these systems, which can be candidates for further pharmacokinetics and in vivo investigations.
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spelling pubmed-104596512023-08-27 Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment de Oliveira, Mariana Carla Balbinot, Rodolfo Bento Villa Nova, Mônica Gonçalves, Renato Sonchini Bidóia, Danielle Lazarin Caetano, Wilker Nakamura, Celso Vataru Bruschi, Marcos Luciano Pharmaceutics Article Leishmaniasis is a disease caused by protozoa species of the Leishmania genus, and the current treatments face several difficulties and obstacles. Most anti-leishmanial drugs are administered intravenously, showing many side effects and drug resistance. The discovery of new anti-leishmanial compounds and the development of new pharmaceutical systems for more efficient and safer treatments are necessary. Copaiba oil-resin (CO) has been shown to be a promising natural compound against leishmaniasis. However, CO displays poor aqueous solubility and bioavailability. Self-emulsifying drug delivery systems (SEDDS) can provide platforms for release of hydrophobic compounds in the gastrointestinal tract, improving their aqueous solubilization, absorption and bioavailability. Therefore, the present work aimed to develop SEDDS containing CO and Soluplus(®) surfactant for the oral treatment of leishmaniasis. The design of the systems was accomplished using ternary phase diagrams. Emulsification and dispersion time tests were used to investigate the emulsification process in gastric and intestinal environments. The formulations were nanostructured and improved the CO solubilization. Their in vitro antiproliferative activity against promastigote forms of L. amazonensis and L. infantum, and low in vitro cytotoxicity against macrophages were also observed. More studies are necessary to determine effectiveness of SOL in these systems, which can be candidates for further pharmacokinetics and in vivo investigations. MDPI 2023-08-12 /pmc/articles/PMC10459651/ /pubmed/37631341 http://dx.doi.org/10.3390/pharmaceutics15082127 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
de Oliveira, Mariana Carla
Balbinot, Rodolfo Bento
Villa Nova, Mônica
Gonçalves, Renato Sonchini
Bidóia, Danielle Lazarin
Caetano, Wilker
Nakamura, Celso Vataru
Bruschi, Marcos Luciano
Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title_full Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title_fullStr Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title_full_unstemmed Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title_short Development of Environmentally Responsive Self-Emulsifying System Containing Copaiba Oil-Resin for Leishmaniasis Oral Treatment
title_sort development of environmentally responsive self-emulsifying system containing copaiba oil-resin for leishmaniasis oral treatment
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10459651/
https://www.ncbi.nlm.nih.gov/pubmed/37631341
http://dx.doi.org/10.3390/pharmaceutics15082127
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