Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis

Detalhes bibliográficos
Autor(a) principal: Jesus, Jéssica Adriana
Data de Publicação: 2021
Outros Autores: Sousa, Ilza Maria Oliveira, da Silva, Thays Nicolli Fragoso, Ferreira, Aurea Favero, Laurenti, Márcia Dalastra, Antonangelo, Leila, Faria, Caroline Silvério, da Costa, Paulo Cardoso, de Carvalho Ferreira, Domingos, Passero, Luiz Felipe Domingues [UNESP]
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.3390/pharmaceutics13060908
http://hdl.handle.net/11449/229082
Resumo: Ursolic acid, a triterpene produced by plants, displayed leishmanicidal activity in vitro and in vivo; however, the low solubility of this triterpene limits its efficacy. To increase the activity of ursolic acid (UA), this triterpene was entrapped in nanostructured lipid carriers (UA-NLC), physical-chemical parameters were estimated, the toxicity was assayed in healthy golden hamsters, and the efficacy of UA-NLC was studied in experimental visceral leishmanisis. UA-NLC exhibited a spherical shape with a smooth surface with a size of 266 nm. UA-NLC displayed low polydispersity (PDI = 0.18) and good colloidal stability (−29.26 mV). Hamsters treated with UA-NLC did not present morphological changes in visceral organs, and the levels of AST, ALT, urea and creatinine were normal. Animals infected with Leishmania (Leishmania) infantum and treated with UA-NLC showed lower parasitism than the infected controls, animals treated with UA or Amphotericin B (AmB). The therapeutic activity of UA-NLC was associated with the increase in a protective immune response, and it was associated with a high degree of spleen and liver preservation, and the normalization of hepatic and renal functions. These data indicate that the use of lipid nanoparticles as UA carriers can be an interesting strategy for the treatment of leishmaniasis.
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spelling Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasisNanoparticlesNanostructured lipid carriersToxicityUrsolic acidVisceral leishmaniasisUrsolic acid, a triterpene produced by plants, displayed leishmanicidal activity in vitro and in vivo; however, the low solubility of this triterpene limits its efficacy. To increase the activity of ursolic acid (UA), this triterpene was entrapped in nanostructured lipid carriers (UA-NLC), physical-chemical parameters were estimated, the toxicity was assayed in healthy golden hamsters, and the efficacy of UA-NLC was studied in experimental visceral leishmanisis. UA-NLC exhibited a spherical shape with a smooth surface with a size of 266 nm. UA-NLC displayed low polydispersity (PDI = 0.18) and good colloidal stability (−29.26 mV). Hamsters treated with UA-NLC did not present morphological changes in visceral organs, and the levels of AST, ALT, urea and creatinine were normal. Animals infected with Leishmania (Leishmania) infantum and treated with UA-NLC showed lower parasitism than the infected controls, animals treated with UA or Amphotericin B (AmB). The therapeutic activity of UA-NLC was associated with the increase in a protective immune response, and it was associated with a high degree of spleen and liver preservation, and the normalization of hepatic and renal functions. These data indicate that the use of lipid nanoparticles as UA carriers can be an interesting strategy for the treatment of leishmaniasis.Laboratório de Patologia e Doenças Infecciosas (LIM50) Departamento de Patologia Faculdade de Medicina da Universidade de São Paulo, Av. Dr. Arnaldo, 455-Cerqueira CésarFaculty of Medical Sciences University of Campinas-UNICAMP, Rua Tessália Vieira de Camargo, 126Laboratório de Patologia Clínica Departamento de Patologia Hospital das Clinicas Faculdade de Medicina da Universidade de São Paulo, Av. Dr. Enéas Carvalho de Aguiar, 155-Cerqueira CésarLaboratório de Investigação Médica (LIM03) Hospital das Clínicas Faculdade de Medicina Universidade de São Paulo, Av. Dr. Arnaldo, 455-Cerqueira CésarUCIBIO REQUIMTE MEDTECH Laboratory of Pharmaceutical Technology Department of Drug Sciences Faculty of Pharmacy University of Porto, Rua Jorge de Viterbo Ferreira, 228Institute of Biosciences São Paulo State University (UNESP), Praça Infante Dom Henrique, s/n, São VicenteInstitute for Advanced Studies of Ocean São Paulo State University (UNESP), Rua João Francisco Bensdorp, 1178, São VicenteInstitute of Biosciences São Paulo State University (UNESP), Praça Infante Dom Henrique, s/n, São VicenteInstitute for Advanced Studies of Ocean São Paulo State University (UNESP), Rua João Francisco Bensdorp, 1178, São VicenteUniversidade de São Paulo (USP)Universidade Estadual de Campinas (UNICAMP)University of PortoUniversidade Estadual Paulista (UNESP)Jesus, Jéssica AdrianaSousa, Ilza Maria Oliveirada Silva, Thays Nicolli FragosoFerreira, Aurea FaveroLaurenti, Márcia DalastraAntonangelo, LeilaFaria, Caroline Silvérioda Costa, Paulo Cardosode Carvalho Ferreira, DomingosPassero, Luiz Felipe Domingues [UNESP]2022-04-29T08:30:17Z2022-04-29T08:30:17Z2021-06-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.3390/pharmaceutics13060908Pharmaceutics, v. 13, n. 6, 2021.1999-4923http://hdl.handle.net/11449/22908210.3390/pharmaceutics130609082-s2.0-85109114416Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengPharmaceuticsinfo:eu-repo/semantics/openAccess2022-04-29T08:30:17Zoai:repositorio.unesp.br:11449/229082Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462022-04-29T08:30:17Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
title Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
spellingShingle Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
Jesus, Jéssica Adriana
Nanoparticles
Nanostructured lipid carriers
Toxicity
Ursolic acid
Visceral leishmaniasis
title_short Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
title_full Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
title_fullStr Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
title_full_unstemmed Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
title_sort Preclinical assessment of ursolic acid loaded into nanostructured lipid carriers in experimental visceral leishmaniasis
author Jesus, Jéssica Adriana
author_facet Jesus, Jéssica Adriana
Sousa, Ilza Maria Oliveira
da Silva, Thays Nicolli Fragoso
Ferreira, Aurea Favero
Laurenti, Márcia Dalastra
Antonangelo, Leila
Faria, Caroline Silvério
da Costa, Paulo Cardoso
de Carvalho Ferreira, Domingos
Passero, Luiz Felipe Domingues [UNESP]
author_role author
author2 Sousa, Ilza Maria Oliveira
da Silva, Thays Nicolli Fragoso
Ferreira, Aurea Favero
Laurenti, Márcia Dalastra
Antonangelo, Leila
Faria, Caroline Silvério
da Costa, Paulo Cardoso
de Carvalho Ferreira, Domingos
Passero, Luiz Felipe Domingues [UNESP]
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade de São Paulo (USP)
Universidade Estadual de Campinas (UNICAMP)
University of Porto
Universidade Estadual Paulista (UNESP)
dc.contributor.author.fl_str_mv Jesus, Jéssica Adriana
Sousa, Ilza Maria Oliveira
da Silva, Thays Nicolli Fragoso
Ferreira, Aurea Favero
Laurenti, Márcia Dalastra
Antonangelo, Leila
Faria, Caroline Silvério
da Costa, Paulo Cardoso
de Carvalho Ferreira, Domingos
Passero, Luiz Felipe Domingues [UNESP]
dc.subject.por.fl_str_mv Nanoparticles
Nanostructured lipid carriers
Toxicity
Ursolic acid
Visceral leishmaniasis
topic Nanoparticles
Nanostructured lipid carriers
Toxicity
Ursolic acid
Visceral leishmaniasis
description Ursolic acid, a triterpene produced by plants, displayed leishmanicidal activity in vitro and in vivo; however, the low solubility of this triterpene limits its efficacy. To increase the activity of ursolic acid (UA), this triterpene was entrapped in nanostructured lipid carriers (UA-NLC), physical-chemical parameters were estimated, the toxicity was assayed in healthy golden hamsters, and the efficacy of UA-NLC was studied in experimental visceral leishmanisis. UA-NLC exhibited a spherical shape with a smooth surface with a size of 266 nm. UA-NLC displayed low polydispersity (PDI = 0.18) and good colloidal stability (−29.26 mV). Hamsters treated with UA-NLC did not present morphological changes in visceral organs, and the levels of AST, ALT, urea and creatinine were normal. Animals infected with Leishmania (Leishmania) infantum and treated with UA-NLC showed lower parasitism than the infected controls, animals treated with UA or Amphotericin B (AmB). The therapeutic activity of UA-NLC was associated with the increase in a protective immune response, and it was associated with a high degree of spleen and liver preservation, and the normalization of hepatic and renal functions. These data indicate that the use of lipid nanoparticles as UA carriers can be an interesting strategy for the treatment of leishmaniasis.
publishDate 2021
dc.date.none.fl_str_mv 2021-06-01
2022-04-29T08:30:17Z
2022-04-29T08:30:17Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.3390/pharmaceutics13060908
Pharmaceutics, v. 13, n. 6, 2021.
1999-4923
http://hdl.handle.net/11449/229082
10.3390/pharmaceutics13060908
2-s2.0-85109114416
url http://dx.doi.org/10.3390/pharmaceutics13060908
http://hdl.handle.net/11449/229082
identifier_str_mv Pharmaceutics, v. 13, n. 6, 2021.
1999-4923
10.3390/pharmaceutics13060908
2-s2.0-85109114416
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Pharmaceutics
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv Scopus
reponame:Repositório Institucional da UNESP
instname:Universidade Estadual Paulista (UNESP)
instacron:UNESP
instname_str Universidade Estadual Paulista (UNESP)
instacron_str UNESP
institution UNESP
reponame_str Repositório Institucional da UNESP
collection Repositório Institucional da UNESP
repository.name.fl_str_mv Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)
repository.mail.fl_str_mv
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