Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties

Autores
Ceschan, Nazareth Eliana; Rosas, Melany Denise; Olivera, María Eugenia; Dugour, Andrea Vanesa; Figueroa, Juan Manuel; Bucala, Veronica; Ramírez Rigo, María Veronica
Año de publicación
2020
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibiotic activity against the bacteria that causes TB (M. tuberculosis). In this work, ionic complexes, composed by hyaluronic acid (HA) and OF, with different neutralization degrees, were prepared and processed by spray drying (SD) to obtain powders for inhalatory administration. Combining a formulation with high neutralization degree, high SD atomization air flowrate and the use of a high-performance collection cyclone, very good process yields were obtained. Carrier-free formulations with a loading of 0.39–0.46 gOF/gpowder showed excellent emitted, fine particle, and respirable fractions for capsule loadings of 25 and 100 mg. The ionic complexes demonstrated higher mucoadhesion than pure OF and HA. The best formulation did not affect CALU-3 cell viability up to a dose 6.5 times higher than the MIC90 reported to treat multi-drug resistant TB.
Fil: Ceschan, Nazareth Eliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Rosas, Melany Denise. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Olivera, María Eugenia. 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. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
Fil: Dugour, Andrea Vanesa. Fundación Pablo Cassará; Argentina
Fil: Figueroa, Juan Manuel. Fundación Pablo Cassará; Argentina
Fil: Bucala, Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Ingeniería Química; Argentina
Fil: Ramírez Rigo, María Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
Materia
CELL VIABILITY
DRUG-EXCIPIENT INTERACTION
FLUOROQUINOLONES
HYALURONIC ACID
INHALATION
MUCOADHESIVE
MULTI-DRUG RESISTANT TUBERCULOSIS
SPRAY DRYING
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:11336/130038
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/130038
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization propertiesCeschan, Nazareth ElianaRosas, Melany DeniseOlivera, María EugeniaDugour, Andrea VanesaFigueroa, Juan ManuelBucala, VeronicaRamírez Rigo, María VeronicaCELL VIABILITYDRUG-EXCIPIENT INTERACTIONFLUOROQUINOLONESHYALURONIC ACIDINHALATIONMUCOADHESIVEMULTI-DRUG RESISTANT TUBERCULOSISSPRAY DRYINGhttps://purl.org/becyt/ford/2.5https://purl.org/becyt/ford/2Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibiotic activity against the bacteria that causes TB (M. tuberculosis). In this work, ionic complexes, composed by hyaluronic acid (HA) and OF, with different neutralization degrees, were prepared and processed by spray drying (SD) to obtain powders for inhalatory administration. Combining a formulation with high neutralization degree, high SD atomization air flowrate and the use of a high-performance collection cyclone, very good process yields were obtained. Carrier-free formulations with a loading of 0.39–0.46 gOF/gpowder showed excellent emitted, fine particle, and respirable fractions for capsule loadings of 25 and 100 mg. The ionic complexes demonstrated higher mucoadhesion than pure OF and HA. The best formulation did not affect CALU-3 cell viability up to a dose 6.5 times higher than the MIC90 reported to treat multi-drug resistant TB.Fil: Ceschan, Nazareth Eliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; ArgentinaFil: Rosas, Melany Denise. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; ArgentinaFil: Olivera, María Eugenia. 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. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; ArgentinaFil: Dugour, Andrea Vanesa. Fundación Pablo Cassará; ArgentinaFil: Figueroa, Juan Manuel. Fundación Pablo Cassará; ArgentinaFil: Bucala, Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Ingeniería Química; ArgentinaFil: Ramírez Rigo, María Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; ArgentinaJohn Wiley & Sons Inc2020-09-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/130038Ceschan, Nazareth Eliana; Rosas, Melany Denise; Olivera, María Eugenia; Dugour, Andrea Vanesa; Figueroa, Juan Manuel; et al.; Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties; John Wiley & Sons Inc; Journal of Pharmaceutical Sciences; 109; 9; 1-9-2020; 2787-27970022-3549CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.xphs.2020.05.027info:eu-repo/semantics/altIdentifier/url/https://jpharmsci.org/article/S0022-3549(20)30304-X/fulltextinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T11:12:08Zoai:ri.conicet.gov.ar:11336/130038instacron: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:34982025-10-22 11:12:08.971CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
title Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
spellingShingle Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
Ceschan, Nazareth Eliana
CELL VIABILITY
DRUG-EXCIPIENT INTERACTION
FLUOROQUINOLONES
HYALURONIC ACID
INHALATION
MUCOADHESIVE
MULTI-DRUG RESISTANT TUBERCULOSIS
SPRAY DRYING
title_short Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
title_full Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
title_fullStr Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
title_full_unstemmed Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
title_sort Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties
dc.creator.none.fl_str_mv Ceschan, Nazareth Eliana
Rosas, Melany Denise
Olivera, María Eugenia
Dugour, Andrea Vanesa
Figueroa, Juan Manuel
Bucala, Veronica
Ramírez Rigo, María Veronica
author Ceschan, Nazareth Eliana
author_facet Ceschan, Nazareth Eliana
Rosas, Melany Denise
Olivera, María Eugenia
Dugour, Andrea Vanesa
Figueroa, Juan Manuel
Bucala, Veronica
Ramírez Rigo, María Veronica
author_role author
author2 Rosas, Melany Denise
Olivera, María Eugenia
Dugour, Andrea Vanesa
Figueroa, Juan Manuel
Bucala, Veronica
Ramírez Rigo, María Veronica
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv CELL VIABILITY
DRUG-EXCIPIENT INTERACTION
FLUOROQUINOLONES
HYALURONIC ACID
INHALATION
MUCOADHESIVE
MULTI-DRUG RESISTANT TUBERCULOSIS
SPRAY DRYING
topic CELL VIABILITY
DRUG-EXCIPIENT INTERACTION
FLUOROQUINOLONES
HYALURONIC ACID
INHALATION
MUCOADHESIVE
MULTI-DRUG RESISTANT TUBERCULOSIS
SPRAY DRYING
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.5
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibiotic activity against the bacteria that causes TB (M. tuberculosis). In this work, ionic complexes, composed by hyaluronic acid (HA) and OF, with different neutralization degrees, were prepared and processed by spray drying (SD) to obtain powders for inhalatory administration. Combining a formulation with high neutralization degree, high SD atomization air flowrate and the use of a high-performance collection cyclone, very good process yields were obtained. Carrier-free formulations with a loading of 0.39–0.46 gOF/gpowder showed excellent emitted, fine particle, and respirable fractions for capsule loadings of 25 and 100 mg. The ionic complexes demonstrated higher mucoadhesion than pure OF and HA. The best formulation did not affect CALU-3 cell viability up to a dose 6.5 times higher than the MIC90 reported to treat multi-drug resistant TB.
Fil: Ceschan, Nazareth Eliana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Rosas, Melany Denise. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Biología, Bioquímica y Farmacia; Argentina
Fil: Olivera, María Eugenia. 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. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
Fil: Dugour, Andrea Vanesa. Fundación Pablo Cassará; Argentina
Fil: Figueroa, Juan Manuel. Fundación Pablo Cassará; Argentina
Fil: Bucala, Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional del Sur. Departamento de Ingeniería Química; Argentina
Fil: Ramírez Rigo, María Veronica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Planta Piloto de Ingeniería Química. Universidad Nacional del Sur. Planta Piloto de Ingeniería Química; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
description Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibiotic activity against the bacteria that causes TB (M. tuberculosis). In this work, ionic complexes, composed by hyaluronic acid (HA) and OF, with different neutralization degrees, were prepared and processed by spray drying (SD) to obtain powders for inhalatory administration. Combining a formulation with high neutralization degree, high SD atomization air flowrate and the use of a high-performance collection cyclone, very good process yields were obtained. Carrier-free formulations with a loading of 0.39–0.46 gOF/gpowder showed excellent emitted, fine particle, and respirable fractions for capsule loadings of 25 and 100 mg. The ionic complexes demonstrated higher mucoadhesion than pure OF and HA. The best formulation did not affect CALU-3 cell viability up to a dose 6.5 times higher than the MIC90 reported to treat multi-drug resistant TB.
publishDate 2020
dc.date.none.fl_str_mv 2020-09-01
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/11336/130038
Ceschan, Nazareth Eliana; Rosas, Melany Denise; Olivera, María Eugenia; Dugour, Andrea Vanesa; Figueroa, Juan Manuel; et al.; Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties; John Wiley & Sons Inc; Journal of Pharmaceutical Sciences; 109; 9; 1-9-2020; 2787-2797
0022-3549
CONICET Digital
CONICET
url http://hdl.handle.net/11336/130038
identifier_str_mv Ceschan, Nazareth Eliana; Rosas, Melany Denise; Olivera, María Eugenia; Dugour, Andrea Vanesa; Figueroa, Juan Manuel; et al.; Development of a carrier-free dry powder ofloxacin formulation with enhanced aerosolization properties; John Wiley & Sons Inc; Journal of Pharmaceutical Sciences; 109; 9; 1-9-2020; 2787-2797
0022-3549
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.xphs.2020.05.027
info:eu-repo/semantics/altIdentifier/url/https://jpharmsci.org/article/S0022-3549(20)30304-X/fulltext
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
application/pdf
dc.publisher.none.fl_str_mv John Wiley & Sons Inc
publisher.none.fl_str_mv John Wiley & Sons Inc
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 12.982451

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