Author | Costa, Amanda Mendonça Barros | |
Author | Silva, Audrey Roouse Soares Tavares | |
Author | Santos, Adriana de Jesus | |
Author | Galvão, Juliana Gouveia | |
Author | Andrade Neto, Valter Viana | |
Author | Santos, Eduardo Caio Torres | |
Author | Ueki, Marcelo Massayoshi | |
Author | Almeida, Luis Eduardo | |
Author | Sarmento, Victor Hugo Vitorino | |
Author | Dolabella, Silvio Santana | |
Author | Scher, Ricardo | |
Author | Lira, Ana Amélia Moreira | |
Author | Nunes, Rogéria de Souza | |
Access date | 2023-05-06T19:10:20Z | |
Available date | 2023-05-06T19:10:20Z | |
Document date | 2023 | |
Citation | COSTA, Amanda Mendonça Barros et al. Acta Tropica, v. 237, p. 1-11, 106744, 2023. | en_US |
ISSN | 0001-706X | en_US |
URI | https://www.arca.fiocruz.br/handle/icict/58190 | |
Language | eng | en_US |
Publisher | Elsevier B.V. | en_US |
Rights | open access | |
Subject in Portuguese | Polímero | en_US |
Subject in Portuguese | Hidrogel | en_US |
Subject in Portuguese | Sistema de entrega de drogas | en_US |
Subject in Portuguese | Citotoxicidade | en_US |
Subject in Portuguese | Leishmaniose | en_US |
Subject in Portuguese | Monoterpeno | en_US |
Title | Thermosensitive system formed by poloxamers containing carvacrol: An effective carrier system against Leishmania amazonensis | en_US |
Type | Article | |
Abstract | The drugs used in the treatment of leishmaniasis show problems concerning side effects and toxicity. As a result,
the search for new actives is necessary, and natural products like carvacrol - 5-isopropyl-2-methylphenol, become a
relevant alternative. To enable the use of carvacrol as an antileishmanial agent, thermosensitive hydrogels were
developed from poloxamer triblock copolymers 407 (P407) and 188 (P188). Carvacrol-free and carvacrolcontaining
hydrogels were obtained from P407 alone and from the mixture of P407 and P188. The hydrogels
were subjected to Differential scanning calorimetry, Small-angle X-ray scattering, Scanning electron microscopy, and
Rheology analysis. The activity of hydrogels and carvacrol isolated against promastigotes and intracellular
amastigotes of Leishmania amazonensis and their cytotoxicity in mammalian cells was determined. The sol-gel
transition temperature for the binary hydrogel containing carvacrol (HG407/188CA) was 37.04 ± 1.35 ◦C.
HG407/188CA presented lamellar structure at temperatures of 25 ◦C and 37 ◦C. HG407/188CA and carvacrol
presented IC50 against Leishmania amazonensis promastigotes of 18.68 ± 1.43 μg/mL and 23.83 ± 3.32 μg/mL,
respectively, and IC50 against Leishmania amazonensis amastigotes of 35.08 ± 0.75 μg/mL and 29.32 ± 0.21 μg/
mL, respectively. HG407/188CA reduced the toxicity of carvacrol in all mammalian cells evaluated, raising the
CC50 in murine peritoneal macrophages from 40.23 ± 0.21 μg/mL to 332.6 ± 4.89 μg/mL, obtaining a Selectivity
Index (SI) of 9.5 against 1.37 of the isolated carvacrol. HG407/188CA provided higher selectivity of carvacrol for
the parasite. Thus, the binary hydrogel obtained may enable the use of carvacrol as a potential antileishmanial
agent. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de janeiro, RJ, Brasil. Rio de Janeiro, RJ, Brasil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de janeiro, RJ, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Ciência e Engenharia de Materiais. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Ciência e Engenharia de Materiais. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Química, Itabaiana, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil / Universidade Federal de Sergipe. Departamento de Morfologia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Morfologia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Affilliation | Universidade Federal de Sergipe. Departamento de Farmácia. São Cristóvão, SE, Brasil. | en_US |
Subject | Polymer | en_US |
Subject | Hydrogel | en_US |
Subject | Drug delivery system | en_US |
Subject | Cytotoxicity | en_US |
Subject | Leishmaniasis | en_US |
Subject | Monoterpene | en_US |
e-ISSN | 10.1016/j.actatropica.2022.106744 | |
Embargo date | 2030 | |