Thermosensitive system formed by poloxamers containing carvacrol: An effective carrier system against Leishmania amazonensis

dc.creatorCosta, Amanda Mendonça Barros
dc.creatorSilva, Audrey Rouse Soares Tavares
dc.creatorSantos, Adriana de Jesus
dc.creatorGalvão, Juliana Gouveia
dc.creatorAndrade Neto, Valter Viana
dc.creatorSantos, Eduardo Caio Torres
dc.creatorUeki, Marcelo Massayoshi
dc.creatorAlmeida, Luis Eduardo
dc.creatorSarmento, Victor Hugo Vitorino
dc.creatorDolabella, Silvio Santana
dc.creatorScher, Ricardo
dc.creatorLira, Ana Amélia Moreira
dc.creatorNunes, Rogéria de Souza
dc.date2023-05-16T12:06:59Z
dc.date2023-05-16T12:06:59Z
dc.date2023
dc.date.accessioned2023-09-26T20:21:30Z
dc.date.available2023-09-26T20:21:30Z
dc.identifierCOSTA, Amanda Mendonça Barros et al. Acta Tropica, v. 237, p. 1-11, 106744, 2023.
dc.identifier0001-706X
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/58423
dc.identifier10.1016/j.actatropica.2022.106744
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8855047
dc.descriptionThe 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.
dc.description2030
dc.formatapplication/pdf
dc.languageeng
dc.publisherElsevier B.V.
dc.rightsrestricted access
dc.subjectPolímero
dc.subjectHydrogel
dc.subjectLeishmaniose
dc.subjectMonoterpeno
dc.subjectSistema de entrega de drogas
dc.subjectCitotoxicidade
dc.subjectPolymer
dc.subjectHydrogel
dc.subjectDrug delivery system
dc.subjectCytotoxicity
dc.subjectLeishmaniasis
dc.subjectMonoterpene
dc.titleThermosensitive system formed by poloxamers containing carvacrol: An effective carrier system against Leishmania amazonensis
dc.typeArticle


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