Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel

Autores
Kolenyak Santos, Fernanda; Garnero, Claudia; De Oliveira, Rosimeire N.; De Souza, Ana L. R.; Chorilli, Marlus; Allegretti, Silmara M.; Longhi, Marcela Raquel; Chaud, Marco V.; Gremião, Maria P.D.
Año de publicación
2015
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.
Fil: Kolenyak Santos, Fernanda. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Garnero, Claudia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: De Oliveira, Rosimeire N.. Universidade Estadual de Campinas; Brasil
Fil: De Souza, Ana L. R.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Chorilli, Marlus. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Allegretti, Silmara M.. Universidade Estadual de Campinas; Brasil
Fil: Longhi, Marcela Raquel. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Chaud, Marco V.. Universidade de Sorocaba; Brasil
Fil: Gremião, Maria P.D.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Materia
Biological Activity
Drug Delivery System
Nanostructured Lipid Carriers
Praziquantel
S. Mansoni
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/38567
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/38567
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of PraziquantelKolenyak Santos, FernandaGarnero, ClaudiaDe Oliveira, Rosimeire N.De Souza, Ana L. R.Chorilli, MarlusAllegretti, Silmara M.Longhi, Marcela RaquelChaud, Marco V.Gremião, Maria P.D.Biological ActivityDrug Delivery SystemNanostructured Lipid CarriersPraziquantelS. Mansonihttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.Fil: Kolenyak Santos, Fernanda. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Garnero, Claudia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: De Oliveira, Rosimeire N.. Universidade Estadual de Campinas; BrasilFil: De Souza, Ana L. R.. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Chorilli, Marlus. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilFil: Allegretti, Silmara M.. Universidade Estadual de Campinas; BrasilFil: Longhi, Marcela Raquel. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Chaud, Marco V.. Universidade de Sorocaba; BrasilFil: Gremião, Maria P.D.. Universidade Estadual Paulista Julio de Mesquita Filho; BrasilAmerican Scientific Publishers2015-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/38567Kolenyak Santos, Fernanda; Garnero, Claudia; De Oliveira, Rosimeire N.; De Souza, Ana L. R.; Chorilli, Marlus; et al.; Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 15; 1; 1-2015; 761-7721533-4880CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1166/jnn.2015.9186info:eu-repo/semantics/altIdentifier/url/http://www.ingentaconnect.com/content/asp/jnn/2015/00000015/00000001/art00141info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T15:42:29Zoai:ri.conicet.gov.ar:11336/38567instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-15 15:42:29.416CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
title Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
spellingShingle Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
Kolenyak Santos, Fernanda
Biological Activity
Drug Delivery System
Nanostructured Lipid Carriers
Praziquantel
S. Mansoni
title_short Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
title_full Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
title_fullStr Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
title_full_unstemmed Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
title_sort Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel
dc.creator.none.fl_str_mv Kolenyak Santos, Fernanda
Garnero, Claudia
De Oliveira, Rosimeire N.
De Souza, Ana L. R.
Chorilli, Marlus
Allegretti, Silmara M.
Longhi, Marcela Raquel
Chaud, Marco V.
Gremião, Maria P.D.
author Kolenyak Santos, Fernanda
author_facet Kolenyak Santos, Fernanda
Garnero, Claudia
De Oliveira, Rosimeire N.
De Souza, Ana L. R.
Chorilli, Marlus
Allegretti, Silmara M.
Longhi, Marcela Raquel
Chaud, Marco V.
Gremião, Maria P.D.
author_role author
author2 Garnero, Claudia
De Oliveira, Rosimeire N.
De Souza, Ana L. R.
Chorilli, Marlus
Allegretti, Silmara M.
Longhi, Marcela Raquel
Chaud, Marco V.
Gremião, Maria P.D.
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Biological Activity
Drug Delivery System
Nanostructured Lipid Carriers
Praziquantel
S. Mansoni
topic Biological Activity
Drug Delivery System
Nanostructured Lipid Carriers
Praziquantel
S. Mansoni
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.
Fil: Kolenyak Santos, Fernanda. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Garnero, Claudia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: De Oliveira, Rosimeire N.. Universidade Estadual de Campinas; Brasil
Fil: De Souza, Ana L. R.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Chorilli, Marlus. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
Fil: Allegretti, Silmara M.. Universidade Estadual de Campinas; Brasil
Fil: Longhi, Marcela Raquel. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Chaud, Marco V.. Universidade de Sorocaba; Brasil
Fil: Gremião, Maria P.D.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil
description Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.
publishDate 2015
dc.date.none.fl_str_mv 2015-01
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/38567
Kolenyak Santos, Fernanda; Garnero, Claudia; De Oliveira, Rosimeire N.; De Souza, Ana L. R.; Chorilli, Marlus; et al.; Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 15; 1; 1-2015; 761-772
1533-4880
CONICET Digital
CONICET
url http://hdl.handle.net/11336/38567
identifier_str_mv Kolenyak Santos, Fernanda; Garnero, Claudia; De Oliveira, Rosimeire N.; De Souza, Ana L. R.; Chorilli, Marlus; et al.; Nanostructured lipid carriers as a strategy to improve the in vitro schistosomiasis activity of Praziquantel; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 15; 1; 1-2015; 761-772
1533-4880
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1166/jnn.2015.9186
info:eu-repo/semantics/altIdentifier/url/http://www.ingentaconnect.com/content/asp/jnn/2015/00000015/00000001/art00141
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv American Scientific Publishers
publisher.none.fl_str_mv American Scientific Publishers
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.22299

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