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dc.contributor.author
Arrua, Eva Carolina
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dc.contributor.author
Hartwig, Olga
dc.contributor.author
Loretz, Brigitta
dc.contributor.author
Goicoechea, Hector Casimiro
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dc.contributor.author
Murgia, Xabier
dc.contributor.author
Lehr, Claus Michael
dc.contributor.author
Salomon, Claudio Javier
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dc.date.available
2023-05-11T17:39:17Z
dc.date.issued
2022-07
dc.identifier.citation
Arrua, Eva Carolina; Hartwig, Olga; Loretz, Brigitta; Goicoechea, Hector Casimiro; Murgia, Xabier; et al.; Improving the oral delivery of benznidazole nanoparticles by optimizing the formulation parameters through a design of experiment and optimization strategy; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 217; 7-2022; 1-9
dc.identifier.issn
0927-7765
dc.identifier.uri
http://hdl.handle.net/11336/197223
dc.description.abstract
Chagas disease is a neglected tropical disease affecting the American continent and also some regions of Europe. Benznidazole, approved by FDA, is a drug of choice but its poor aqueous solubility may lead to a low bioavailability and efficacy. Therefore, the aim of this study was to formulate nanoparticles of benznidazole for improving its solubility, dissolution and permeability. A Plackett–Burman design was applied to identify the effect of 5 factors over 4 responses. Then, a Central Composite design was applied to estimate the values of the most important factors leading to the best compromise between highest nanoprecipitation efficiency, drug solubility and lower particle size. The optimized nanoparticles were evaluated for in vitro drug release in biorelevant media, stability studies and transmission electron microscopy. Biocompatibility and permeability of nanoparticles were evaluated on the Caco-2 cell line. The findings of the optimization process indicated that concentration of drug and stabilizer influenced significantly the particle size while concentration of stabilizer and organic/water phase volume ratio mainly influenced the drug solubility. Stability studies suggested that benznidazole nanoparticles were stable after 12 months at different temperatures. Minimal interactions of those nanoparticles and mucin glycoproteins suggested favorable properties to address the intestinal mucus barrier. Cell viability studies confirmed the safety profile of the optimized formulation and showed an increased permeation through the Caco-2 cells. Thus, this study confirmed the suitability of the design of experiment and optimization approach to elucidate critical parameters influencing the quality of benznidazole nanoparticles, which could lead to a more efficient management of Chagas disease by oral route.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier Science
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
BENZNIDAZOLE
dc.subject
DESIGN OF EXPERIMENT AND OPTIMIZATION
dc.subject
MUCUS INTERACTIONS
dc.subject
NANOPARTICLES
dc.subject
STABILIZER
dc.subject.classification
Otras Ciencias Químicas
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dc.subject.classification
Ciencias Químicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Improving the oral delivery of benznidazole nanoparticles by optimizing the formulation parameters through a design of experiment and optimization strategy
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2023-05-11T14:11:08Z
dc.journal.volume
217
dc.journal.pagination
1-9
dc.journal.pais
Países Bajos
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dc.journal.ciudad
Amsterdam
dc.description.fil
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
dc.description.fil
Fil: Hartwig, Olga. Helmholtz Centre for Infection Research; Alemania
dc.description.fil
Fil: Loretz, Brigitta. Helmholtz Centre for Infection Research; Alemania
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Fil: Goicoechea, Hector Casimiro. Universidad Nacional del Litoral. Facultad de Bioquímica y Ciencias Biológicas. Laboratorio de Desarrollo Analítico y Quimiometría; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe; Argentina
dc.description.fil
Fil: Murgia, Xabier. Helmholtz Centre for Infection Research; Alemania
dc.description.fil
Fil: Lehr, Claus Michael. Helmholtz Centre for Infection Research; Alemania. Universitat Saarland; Alemania
dc.description.fil
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
dc.journal.title
Colloids and Surfaces B: Biointerfaces
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://doi.org/10.1016/j.colsurfb.2022.112678
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