Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?

Autores
Seremeta, Katia Pamela; Arrua, Eva Carolina; Okulik, Nora Beatriz; Salomon, Claudio Javier
Año de publicación
2019
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Benznidazole (BNZ) is the drug of choice for the treatment of Chagas disease in many countries. However, its low water solubility produces low and/or variable oral bioavailability. Thus, the aim of this work was to formulate micro- and nanoparticles based on Eudragit® RS PO and Eudragit® RL PO as a convenient approach to increase the dissolution rate of BNZ. The microparticles were obtained by means of spray-drying process while the nanoparticles were prepared through the nanoprecipitation technique and further freeze-drying. The results indicated that nanoparticles were obtained in 86% yield while microparticles were obtained in 68% yield. In both cases, the encapsulation efficiency of particles was greater than 78% while drug loading capacity was nearly 24% w/w and 18% w/w, after spray-drying and freeze-drying procedures, respectively. Images of scanning electron microscopy showed that the particles obtained by spray-drying and freeze-drying were in the micrometer and nanometer scale, respectively. FT-IR spectra of BNZ-loaded particles obtained by both methods showed characteristic bands of BNZ confirming that part of drug remained on their surface. Thermal analysis revealed that the drug crystallinity after both methods decreased. Physical stability evaluation of the nanoparticles confirmed that Pluronic® F68 was suitable to keep the particles size in a range of 300 nm after 70 days storage at 4 ± 2 °C. In-vitro release studies showed increased dissolution rate of drug from the particles obtained by both methods respect to untreated BNZ. The kinetics of drug release in acid media followed the Higuchi kinetics indicating drug diffusion mechanism from particles.
Fil: Seremeta, Katia Pamela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; Argentina. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina
Fil: Arrua, Eva Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Okulik, Nora Beatriz. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; Argentina
Fil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Materia
EUDRAGIT
DISSOLUTION EFFICIENCY
DRUG DIFUSSION
BENZNIDAZOLE
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/108136
Acceder
id CONICETDig_680c0092314faab8017c52adecdc7f37
oai_identifier_str oai:ri.conicet.gov.ar:11336/108136
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?Seremeta, Katia PamelaArrua, Eva CarolinaOkulik, Nora BeatrizSalomon, Claudio JavierEUDRAGITDISSOLUTION EFFICIENCYDRUG DIFUSSIONBENZNIDAZOLEhttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2Benznidazole (BNZ) is the drug of choice for the treatment of Chagas disease in many countries. However, its low water solubility produces low and/or variable oral bioavailability. Thus, the aim of this work was to formulate micro- and nanoparticles based on Eudragit® RS PO and Eudragit® RL PO as a convenient approach to increase the dissolution rate of BNZ. The microparticles were obtained by means of spray-drying process while the nanoparticles were prepared through the nanoprecipitation technique and further freeze-drying. The results indicated that nanoparticles were obtained in 86% yield while microparticles were obtained in 68% yield. In both cases, the encapsulation efficiency of particles was greater than 78% while drug loading capacity was nearly 24% w/w and 18% w/w, after spray-drying and freeze-drying procedures, respectively. Images of scanning electron microscopy showed that the particles obtained by spray-drying and freeze-drying were in the micrometer and nanometer scale, respectively. FT-IR spectra of BNZ-loaded particles obtained by both methods showed characteristic bands of BNZ confirming that part of drug remained on their surface. Thermal analysis revealed that the drug crystallinity after both methods decreased. Physical stability evaluation of the nanoparticles confirmed that Pluronic® F68 was suitable to keep the particles size in a range of 300 nm after 70 days storage at 4 ± 2 °C. In-vitro release studies showed increased dissolution rate of drug from the particles obtained by both methods respect to untreated BNZ. The kinetics of drug release in acid media followed the Higuchi kinetics indicating drug diffusion mechanism from particles.Fil: Seremeta, Katia Pamela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; Argentina. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; ArgentinaFil: Arrua, Eva Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaFil: Okulik, Nora Beatriz. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; ArgentinaFil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaElsevier Science2019-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/108136Seremeta, Katia Pamela; Arrua, Eva Carolina; Okulik, Nora Beatriz; Salomon, Claudio Javier; Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 177; 1-2019; 169-1770927-7765CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0927776519300384info:eu-repo/semantics/altIdentifier/doi/10.1016/j.colsurfb.2019.01.039info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:43:51Zoai:ri.conicet.gov.ar:11336/108136instacron: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:34982025-09-03 09:43:51.36CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
title Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
spellingShingle Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
Seremeta, Katia Pamela
EUDRAGIT
DISSOLUTION EFFICIENCY
DRUG DIFUSSION
BENZNIDAZOLE
title_short Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
title_full Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
title_fullStr Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
title_full_unstemmed Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
title_sort Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?
dc.creator.none.fl_str_mv Seremeta, Katia Pamela
Arrua, Eva Carolina
Okulik, Nora Beatriz
Salomon, Claudio Javier
author Seremeta, Katia Pamela
author_facet Seremeta, Katia Pamela
Arrua, Eva Carolina
Okulik, Nora Beatriz
Salomon, Claudio Javier
author_role author
author2 Arrua, Eva Carolina
Okulik, Nora Beatriz
Salomon, Claudio Javier
author2_role author
author
author
dc.subject.none.fl_str_mv EUDRAGIT
DISSOLUTION EFFICIENCY
DRUG DIFUSSION
BENZNIDAZOLE
topic EUDRAGIT
DISSOLUTION EFFICIENCY
DRUG DIFUSSION
BENZNIDAZOLE
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv Benznidazole (BNZ) is the drug of choice for the treatment of Chagas disease in many countries. However, its low water solubility produces low and/or variable oral bioavailability. Thus, the aim of this work was to formulate micro- and nanoparticles based on Eudragit® RS PO and Eudragit® RL PO as a convenient approach to increase the dissolution rate of BNZ. The microparticles were obtained by means of spray-drying process while the nanoparticles were prepared through the nanoprecipitation technique and further freeze-drying. The results indicated that nanoparticles were obtained in 86% yield while microparticles were obtained in 68% yield. In both cases, the encapsulation efficiency of particles was greater than 78% while drug loading capacity was nearly 24% w/w and 18% w/w, after spray-drying and freeze-drying procedures, respectively. Images of scanning electron microscopy showed that the particles obtained by spray-drying and freeze-drying were in the micrometer and nanometer scale, respectively. FT-IR spectra of BNZ-loaded particles obtained by both methods showed characteristic bands of BNZ confirming that part of drug remained on their surface. Thermal analysis revealed that the drug crystallinity after both methods decreased. Physical stability evaluation of the nanoparticles confirmed that Pluronic® F68 was suitable to keep the particles size in a range of 300 nm after 70 days storage at 4 ± 2 °C. In-vitro release studies showed increased dissolution rate of drug from the particles obtained by both methods respect to untreated BNZ. The kinetics of drug release in acid media followed the Higuchi kinetics indicating drug diffusion mechanism from particles.
Fil: Seremeta, Katia Pamela. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; Argentina. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina
Fil: Arrua, Eva Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Okulik, Nora Beatriz. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Nordeste; Argentina
Fil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
description Benznidazole (BNZ) is the drug of choice for the treatment of Chagas disease in many countries. However, its low water solubility produces low and/or variable oral bioavailability. Thus, the aim of this work was to formulate micro- and nanoparticles based on Eudragit® RS PO and Eudragit® RL PO as a convenient approach to increase the dissolution rate of BNZ. The microparticles were obtained by means of spray-drying process while the nanoparticles were prepared through the nanoprecipitation technique and further freeze-drying. The results indicated that nanoparticles were obtained in 86% yield while microparticles were obtained in 68% yield. In both cases, the encapsulation efficiency of particles was greater than 78% while drug loading capacity was nearly 24% w/w and 18% w/w, after spray-drying and freeze-drying procedures, respectively. Images of scanning electron microscopy showed that the particles obtained by spray-drying and freeze-drying were in the micrometer and nanometer scale, respectively. FT-IR spectra of BNZ-loaded particles obtained by both methods showed characteristic bands of BNZ confirming that part of drug remained on their surface. Thermal analysis revealed that the drug crystallinity after both methods decreased. Physical stability evaluation of the nanoparticles confirmed that Pluronic® F68 was suitable to keep the particles size in a range of 300 nm after 70 days storage at 4 ± 2 °C. In-vitro release studies showed increased dissolution rate of drug from the particles obtained by both methods respect to untreated BNZ. The kinetics of drug release in acid media followed the Higuchi kinetics indicating drug diffusion mechanism from particles.
publishDate 2019
dc.date.none.fl_str_mv 2019-01
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/11336/108136
Seremeta, Katia Pamela; Arrua, Eva Carolina; Okulik, Nora Beatriz; Salomon, Claudio Javier; Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 177; 1-2019; 169-177
0927-7765
CONICET Digital
CONICET
url http://hdl.handle.net/11336/108136
identifier_str_mv Seremeta, Katia Pamela; Arrua, Eva Carolina; Okulik, Nora Beatriz; Salomon, Claudio Javier; Development and characterization of benznidazole nano- and microparticles: A new tool for pediatric treatment of Chagas disease?; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 177; 1-2019; 169-177
0927-7765
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0927776519300384
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.colsurfb.2019.01.039
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
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
_version_ 1842268627755073536
score 13.13397

Publicaciones similares