Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2020 |
| Outros Autores: | , , , , , , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/42398 |
Resumo: | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. |
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Galvão, Juliana G.Santos, Raquel L.Silva, Audrey R. S. T.Santos, Jeferson S.Costa, Amanda M. B.Chandasana, HardikAndrade Neto, Valter V.Santos, Eduardo Caio TorresLira, Ana Amélia M.Dolabella, SilvioScher, RicardoKima, Peter E.Derendorf, HartmutNunes, Rogéria S.2020-07-25T19:19:00Z2020-07-25T19:19:00Z2020GALVÃO, Juliana G. et al. Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment. European Journal of Pharmaceutical Sciences, v. 150, p. 1-12, Apr. 2020.0928-0987https://www.arca.fiocruz.br/handle/icict/4239810.1016/j.ejps.2020.1053351879-0720engElsevier 12 MonthsLeishmaniaLipídios sólidosMonoterpeno fenólicoProdutos naturaisNanomedicinaTratamento intravenosoSolid lipidsPhenolic monoterpeneNatural productsLeishmaniaNanomedicineIntravenous treatmentCarvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatmentinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.Universidade Federal de Sergipe. Departamento de Morfologia. São Cristóvao. SE, Brasil.Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.University of Florida, Department of Pharmaceutics. FL, USA.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanosomatídeos. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanosomatídeos. Rio de Janeiro, RJ, Brasil.Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.Universidade Federal de Sergipe. Departamento de Morfologia. São Cristóvao. SE, Brasil.Universidade Federal de Sergipe. Departamento de Morfologia. São Cristóvao. SE, Brasil.University of Florida. Department of Microbiology and Cell Science. FL, USA.University of Florida, Department of Pharmaceutics. FL, USA.Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil.Leishmaniasis are a group of neglected infectious diseases caused by protozoa of the genus Leishmania with distinct presentations. The available leishmaniasis treatment options are either expensive and/or; cause adverse effects and some are ineffective for resistant Leishmania strains. Therefore, molecules derived from natural products as the monoterpene carvacrol, have attracted interest as promising anti-leishmania agents. However, the therapeutic use of carvacrol is limited due to its low aqueous solubility, rapid oxidation and volatilization. Thus, the development of nanostructured lipid carriers (NLCs) was proposed in the present study as a promising nanotechnology strategy to overcome these limitations and enable the use of carvacrol in leishmaniasis therapy. Carvacrol NLCs were obtained using a warm microemulsion method, and evaluated regarding the influence of lipid matrix and components concentration on the NLCs formation. NLCs were characterized by DSC and XRD as well. In addition, to the in vitro carvacrol release from NLCs, the in vitro cytotoxicity and leishmanicidal activity assays, and the in vivo pharmacokinetics evaluation of free and encapsulated carvacrol were performed. NLCs containing carvacrol were obtained successfully using a warm microemulsion dilution method. The NLCs formulation with the lowest particle size (98.42 ± 0.80 nm), narrowest size distribution (suitable for intravenous administration), and the highest encapsulation efficiency was produced by using beeswax as solid lipid (HLB=9) and 5% of lipids and surfactant. The in vitro release of carvacrol from NLCs was fitted to the Korsmeyer and Peppas, and Weibull models, demonstrating that the release mechanism is probably the Fickian diffusion type. Moreover, carvacrol encapsulation in NLCs provided a lower cytotoxicity in comparison to free carvacrol (p<0.05), increasing its in vitro leishmanicidal efficacy in the amastigote form. Finally, the in vivo pharmacokinetics of carvacrol after IV bolus administration suggests that this phenolic monoterpene undergoes enterohepatic circulation and therefore presented a long half-life (t1/2) and low clearance (Cl). In addition, C0, mean residence time (MRT) and Vdss of encapsulated carvacrol were higher than free carvacrol (p < 0.05), favoring a higher distribution of carvacrol in the target tissues. Thus, it is possible to conclude that the developed NLCs are a promising delivery system for leishmaniasis treatment.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/42398/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdfValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdfapplication/pdf5616812https://www.arca.fiocruz.br/bitstream/icict/42398/2/ValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdf0b34d6ae2453d423f6dce8b721a7b6beMD52TEXTValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdf.txtValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdf.txtExtracted texttext/plain72013https://www.arca.fiocruz.br/bitstream/icict/42398/3/ValterVAndradeNeto_EduarcoCTSantos_etal_IOC_2020.pdf.txtce7cbb124c13449af151fdfe80672142MD53icict/423982023-09-05 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| dc.title.pt_BR.fl_str_mv |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| title |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| spellingShingle |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment Galvão, Juliana G. Leishmania Lipídios sólidos Monoterpeno fenólico Produtos naturais Nanomedicina Tratamento intravenoso Solid lipids Phenolic monoterpene Natural products Leishmania Nanomedicine Intravenous treatment |
| title_short |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| title_full |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| title_fullStr |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| title_full_unstemmed |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| title_sort |
Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment |
| author |
Galvão, Juliana G. |
| author_facet |
Galvão, Juliana G. Santos, Raquel L. Silva, Audrey R. S. T. Santos, Jeferson S. Costa, Amanda M. B. Chandasana, Hardik Andrade Neto, Valter V. Santos, Eduardo Caio Torres Lira, Ana Amélia M. Dolabella, Silvio Scher, Ricardo Kima, Peter E. Derendorf, Hartmut Nunes, Rogéria S. |
| author_role |
author |
| author2 |
Santos, Raquel L. Silva, Audrey R. S. T. Santos, Jeferson S. Costa, Amanda M. B. Chandasana, Hardik Andrade Neto, Valter V. Santos, Eduardo Caio Torres Lira, Ana Amélia M. Dolabella, Silvio Scher, Ricardo Kima, Peter E. Derendorf, Hartmut Nunes, Rogéria S. |
| author2_role |
author author author author author author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Galvão, Juliana G. Santos, Raquel L. Silva, Audrey R. S. T. Santos, Jeferson S. Costa, Amanda M. B. Chandasana, Hardik Andrade Neto, Valter V. Santos, Eduardo Caio Torres Lira, Ana Amélia M. Dolabella, Silvio Scher, Ricardo Kima, Peter E. Derendorf, Hartmut Nunes, Rogéria S. |
| dc.subject.other.pt_BR.fl_str_mv |
Leishmania Lipídios sólidos Monoterpeno fenólico Produtos naturais Nanomedicina Tratamento intravenoso |
| topic |
Leishmania Lipídios sólidos Monoterpeno fenólico Produtos naturais Nanomedicina Tratamento intravenoso Solid lipids Phenolic monoterpene Natural products Leishmania Nanomedicine Intravenous treatment |
| dc.subject.en.pt_BR.fl_str_mv |
Solid lipids Phenolic monoterpene Natural products Leishmania Nanomedicine Intravenous treatment |
| description |
Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. |
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2020 |
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2020-07-25T19:19:00Z |
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2020-07-25T19:19:00Z |
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2020 |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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GALVÃO, Juliana G. et al. Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment. European Journal of Pharmaceutical Sciences, v. 150, p. 1-12, Apr. 2020. |
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https://www.arca.fiocruz.br/handle/icict/42398 |
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0928-0987 |
| dc.identifier.doi.none.fl_str_mv |
10.1016/j.ejps.2020.105335 |
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1879-0720 |
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GALVÃO, Juliana G. et al. Carvacrol loaded nanostructured lipid carriers as a promising parenteral formulation for leishmaniasis treatment. European Journal of Pharmaceutical Sciences, v. 150, p. 1-12, Apr. 2020. 0928-0987 10.1016/j.ejps.2020.105335 1879-0720 |
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Elsevier 12 Months |
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Elsevier 12 Months |
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