Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of th...

Autores
Mura, Paola A.; Cirri, Marzia; Rossetti, Cristian Alan; Allemandi, Daniel Alberto; Paredes, Alejandro Javier; Palma, Santiago Daniel
Año de publicación
2024
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
The effectiveness of dry-ball and wet-bead nano-milling methods in producing nanocrystals of glyburide with increased dissolution rate has been compared. A full factorial design was applied to both methods to systematically evaluate the effect of the most critical factors (milling time, milling speed, ball/bead volume, drug amount) on the responses to be optimized (particle size and dissolution rate). Different experimental conditions were found to obtain the best results: the dry-method required to increase frequency and milling time and reduce ball volume and drug amount, while the wet-method to increase milling rate and drug amount and reduce bead volume and milling time. The results obtained under the respective optimal conditions evidenced a similar performance in nanocrystal production (120 and 180 nm for dry-ball and wet-bead milling, respectively) while a higher % dissolved at 10 min (28 vs 14 %) was found for the wet-method, principally ascribed to the presence, in this case, of the solubilizing polymer P188, added as stabilizer. Differently from the wet-method, the dry-method showed no direct relationship between particle size reduction and drug dissolution rate increase. Solid-state studies evidenced a role of the drug crystallinity loss, caused by the dry-milling, in affecting dissolution rate and proved the stability of the drug under both the milling processes.
Fil: Mura, Paola A.. Università degli Studi di Firenze; Italia
Fil: Cirri, Marzia. Università degli Studi di Firenze; Italia
Fil: Rossetti, Cristian Alan. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Paredes, Alejandro Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina. The Queens University of Belfast; Irlanda
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Materia
Dry-milling rate
Glyburide
Wet-milling
Nanocrystals
Dissolution
Experimental design
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/261991

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spelling Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methodsMura, Paola A.Cirri, MarziaRossetti, Cristian AlanAllemandi, Daniel AlbertoParedes, Alejandro JavierPalma, Santiago DanielDry-milling rateGlyburideWet-millingNanocrystalsDissolutionExperimental designhttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2The effectiveness of dry-ball and wet-bead nano-milling methods in producing nanocrystals of glyburide with increased dissolution rate has been compared. A full factorial design was applied to both methods to systematically evaluate the effect of the most critical factors (milling time, milling speed, ball/bead volume, drug amount) on the responses to be optimized (particle size and dissolution rate). Different experimental conditions were found to obtain the best results: the dry-method required to increase frequency and milling time and reduce ball volume and drug amount, while the wet-method to increase milling rate and drug amount and reduce bead volume and milling time. The results obtained under the respective optimal conditions evidenced a similar performance in nanocrystal production (120 and 180 nm for dry-ball and wet-bead milling, respectively) while a higher % dissolved at 10 min (28 vs 14 %) was found for the wet-method, principally ascribed to the presence, in this case, of the solubilizing polymer P188, added as stabilizer. Differently from the wet-method, the dry-method showed no direct relationship between particle size reduction and drug dissolution rate increase. Solid-state studies evidenced a role of the drug crystallinity loss, caused by the dry-milling, in affecting dissolution rate and proved the stability of the drug under both the milling processes.Fil: Mura, Paola A.. Università degli Studi di Firenze; ItaliaFil: Cirri, Marzia. Università degli Studi di Firenze; ItaliaFil: Rossetti, Cristian Alan. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Paredes, Alejandro Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina. The Queens University of Belfast; IrlandaFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaElsevier2024-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/261991Mura, Paola A.; Cirri, Marzia; Rossetti, Cristian Alan; Allemandi, Daniel Alberto; Paredes, Alejandro Javier; et al.; Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods; Elsevier; Journal of Drug Delivery Science and Technology; 91; 1-2024; 1-121773-2247CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://linkinghub.elsevier.com/retrieve/pii/S1773224723010742info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jddst.2023.105222info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-10T13:10:05Zoai:ri.conicet.gov.ar:11336/261991instacron: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:34982025-09-10 13:10:05.587CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
title Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
spellingShingle Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
Mura, Paola A.
Dry-milling rate
Glyburide
Wet-milling
Nanocrystals
Dissolution
Experimental design
title_short Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
title_full Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
title_fullStr Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
title_full_unstemmed Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
title_sort Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods
dc.creator.none.fl_str_mv Mura, Paola A.
Cirri, Marzia
Rossetti, Cristian Alan
Allemandi, Daniel Alberto
Paredes, Alejandro Javier
Palma, Santiago Daniel
author Mura, Paola A.
author_facet Mura, Paola A.
Cirri, Marzia
Rossetti, Cristian Alan
Allemandi, Daniel Alberto
Paredes, Alejandro Javier
Palma, Santiago Daniel
author_role author
author2 Cirri, Marzia
Rossetti, Cristian Alan
Allemandi, Daniel Alberto
Paredes, Alejandro Javier
Palma, Santiago Daniel
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Dry-milling rate
Glyburide
Wet-milling
Nanocrystals
Dissolution
Experimental design
topic Dry-milling rate
Glyburide
Wet-milling
Nanocrystals
Dissolution
Experimental design
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv The effectiveness of dry-ball and wet-bead nano-milling methods in producing nanocrystals of glyburide with increased dissolution rate has been compared. A full factorial design was applied to both methods to systematically evaluate the effect of the most critical factors (milling time, milling speed, ball/bead volume, drug amount) on the responses to be optimized (particle size and dissolution rate). Different experimental conditions were found to obtain the best results: the dry-method required to increase frequency and milling time and reduce ball volume and drug amount, while the wet-method to increase milling rate and drug amount and reduce bead volume and milling time. The results obtained under the respective optimal conditions evidenced a similar performance in nanocrystal production (120 and 180 nm for dry-ball and wet-bead milling, respectively) while a higher % dissolved at 10 min (28 vs 14 %) was found for the wet-method, principally ascribed to the presence, in this case, of the solubilizing polymer P188, added as stabilizer. Differently from the wet-method, the dry-method showed no direct relationship between particle size reduction and drug dissolution rate increase. Solid-state studies evidenced a role of the drug crystallinity loss, caused by the dry-milling, in affecting dissolution rate and proved the stability of the drug under both the milling processes.
Fil: Mura, Paola A.. Università degli Studi di Firenze; Italia
Fil: Cirri, Marzia. Università degli Studi di Firenze; Italia
Fil: Rossetti, Cristian Alan. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Paredes, Alejandro Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina. The Queens University of Belfast; Irlanda
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
description The effectiveness of dry-ball and wet-bead nano-milling methods in producing nanocrystals of glyburide with increased dissolution rate has been compared. A full factorial design was applied to both methods to systematically evaluate the effect of the most critical factors (milling time, milling speed, ball/bead volume, drug amount) on the responses to be optimized (particle size and dissolution rate). Different experimental conditions were found to obtain the best results: the dry-method required to increase frequency and milling time and reduce ball volume and drug amount, while the wet-method to increase milling rate and drug amount and reduce bead volume and milling time. The results obtained under the respective optimal conditions evidenced a similar performance in nanocrystal production (120 and 180 nm for dry-ball and wet-bead milling, respectively) while a higher % dissolved at 10 min (28 vs 14 %) was found for the wet-method, principally ascribed to the presence, in this case, of the solubilizing polymer P188, added as stabilizer. Differently from the wet-method, the dry-method showed no direct relationship between particle size reduction and drug dissolution rate increase. Solid-state studies evidenced a role of the drug crystallinity loss, caused by the dry-milling, in affecting dissolution rate and proved the stability of the drug under both the milling processes.
publishDate 2024
dc.date.none.fl_str_mv 2024-01
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/11336/261991
Mura, Paola A.; Cirri, Marzia; Rossetti, Cristian Alan; Allemandi, Daniel Alberto; Paredes, Alejandro Javier; et al.; Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods; Elsevier; Journal of Drug Delivery Science and Technology; 91; 1-2024; 1-12
1773-2247
CONICET Digital
CONICET
url http://hdl.handle.net/11336/261991
identifier_str_mv Mura, Paola A.; Cirri, Marzia; Rossetti, Cristian Alan; Allemandi, Daniel Alberto; Paredes, Alejandro Javier; et al.; Preparation of glyburide nanocrystals with improved dissolution properties by dry-ball- and wet-bead- milling: Systematic comparison by experimental design of the performance of the two methods; Elsevier; Journal of Drug Delivery Science and Technology; 91; 1-2024; 1-12
1773-2247
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://linkinghub.elsevier.com/retrieve/pii/S1773224723010742
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jddst.2023.105222
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
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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