Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization

Autores
Calvo, Natalia Lorena; Tejada Jacob, Guillermo Ivan; Svetaz, Laura Andrea; Quiroga, Ariel Dario; Alvarez, Vera Alejandra; Lamas, Maria Celina; Leonardi, Darío
Año de publicación
2021
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients’ comfort and compliance, were considered. Mechanical testing, such as load at break, elongation at break, and mucoadhesive strength were also included as dependent variables. The optimal mucoadhesive film formulation, which should be obtained at a drying temperature of 30 °C, was found to include the combination of CH and HPMC (forming polymers) at 0.25:0.75 ratio, a mixture of polyethylene glycol 400 and propylene glycol as plasticizers (0.07:0.93, 5% w/w), and TCZ loaded at 15 % w/w. The optimal preparation was subjected to exhaustive characterization studies, which revealed that the drug was entrapped in the polymeric matrix in an amorphous state and that the film exhibited a smooth and uniform surface, demonstrating excellent component compatibility. In vitro tests showed that the formulation has an excellent time to kill value (3 min) and lacks cytotoxicity, suggesting that it should be highly effective and safe.
Fil: Calvo, Natalia Lorena. 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: Tejada Jacob, Guillermo Ivan. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario; Argentina
Fil: Svetaz, Laura Andrea. Universidad Nacional de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Quiroga, Ariel Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; Argentina
Fil: Alvarez, Vera Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; Argentina
Fil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina
Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina. Universidad Nacional de Rosario; Argentina
Materia
CHITOSAN
EXPERIMENTAL DESIGN OPTIMIZATION
HYDROXYPROPYL METHYLCELLULOSE
TIOCONAZOLE
VAGINAL FILM
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:11336/211988
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/211988
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterizationCalvo, Natalia LorenaTejada Jacob, Guillermo IvanSvetaz, Laura AndreaQuiroga, Ariel DarioAlvarez, Vera AlejandraLamas, Maria CelinaLeonardi, DaríoCHITOSANEXPERIMENTAL DESIGN OPTIMIZATIONHYDROXYPROPYL METHYLCELLULOSETIOCONAZOLEVAGINAL FILMhttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients’ comfort and compliance, were considered. Mechanical testing, such as load at break, elongation at break, and mucoadhesive strength were also included as dependent variables. The optimal mucoadhesive film formulation, which should be obtained at a drying temperature of 30 °C, was found to include the combination of CH and HPMC (forming polymers) at 0.25:0.75 ratio, a mixture of polyethylene glycol 400 and propylene glycol as plasticizers (0.07:0.93, 5% w/w), and TCZ loaded at 15 % w/w. The optimal preparation was subjected to exhaustive characterization studies, which revealed that the drug was entrapped in the polymeric matrix in an amorphous state and that the film exhibited a smooth and uniform surface, demonstrating excellent component compatibility. In vitro tests showed that the formulation has an excellent time to kill value (3 min) and lacks cytotoxicity, suggesting that it should be highly effective and safe.Fil: Calvo, Natalia Lorena. 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: Tejada Jacob, Guillermo Ivan. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario; ArgentinaFil: Svetaz, Laura Andrea. Universidad Nacional de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Quiroga, Ariel Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; ArgentinaFil: Alvarez, Vera Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; ArgentinaFil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; ArgentinaFil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina. Universidad Nacional de Rosario; ArgentinaElsevier Science2021-10info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/211988Calvo, Natalia Lorena; Tejada Jacob, Guillermo Ivan; Svetaz, Laura Andrea; Quiroga, Ariel Dario; Alvarez, Vera Alejandra; et al.; Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization; Elsevier Science; Journal of Pharmaceutical and Biomedical Analysis; 205; 10-2021; 1-370731-7085CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://linkinghub.elsevier.com/retrieve/pii/S0731708521004143info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jpba.2021.114303info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T11:39:17Zoai:ri.conicet.gov.ar:11336/211988instacron: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 11:39:18.215CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
title Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
spellingShingle Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
Calvo, Natalia Lorena
CHITOSAN
EXPERIMENTAL DESIGN OPTIMIZATION
HYDROXYPROPYL METHYLCELLULOSE
TIOCONAZOLE
VAGINAL FILM
title_short Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
title_full Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
title_fullStr Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
title_full_unstemmed Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
title_sort Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization
dc.creator.none.fl_str_mv Calvo, Natalia Lorena
Tejada Jacob, Guillermo Ivan
Svetaz, Laura Andrea
Quiroga, Ariel Dario
Alvarez, Vera Alejandra
Lamas, Maria Celina
Leonardi, Darío
author Calvo, Natalia Lorena
author_facet Calvo, Natalia Lorena
Tejada Jacob, Guillermo Ivan
Svetaz, Laura Andrea
Quiroga, Ariel Dario
Alvarez, Vera Alejandra
Lamas, Maria Celina
Leonardi, Darío
author_role author
author2 Tejada Jacob, Guillermo Ivan
Svetaz, Laura Andrea
Quiroga, Ariel Dario
Alvarez, Vera Alejandra
Lamas, Maria Celina
Leonardi, Darío
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv CHITOSAN
EXPERIMENTAL DESIGN OPTIMIZATION
HYDROXYPROPYL METHYLCELLULOSE
TIOCONAZOLE
VAGINAL FILM
topic CHITOSAN
EXPERIMENTAL DESIGN OPTIMIZATION
HYDROXYPROPYL METHYLCELLULOSE
TIOCONAZOLE
VAGINAL FILM
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients’ comfort and compliance, were considered. Mechanical testing, such as load at break, elongation at break, and mucoadhesive strength were also included as dependent variables. The optimal mucoadhesive film formulation, which should be obtained at a drying temperature of 30 °C, was found to include the combination of CH and HPMC (forming polymers) at 0.25:0.75 ratio, a mixture of polyethylene glycol 400 and propylene glycol as plasticizers (0.07:0.93, 5% w/w), and TCZ loaded at 15 % w/w. The optimal preparation was subjected to exhaustive characterization studies, which revealed that the drug was entrapped in the polymeric matrix in an amorphous state and that the film exhibited a smooth and uniform surface, demonstrating excellent component compatibility. In vitro tests showed that the formulation has an excellent time to kill value (3 min) and lacks cytotoxicity, suggesting that it should be highly effective and safe.
Fil: Calvo, Natalia Lorena. 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: Tejada Jacob, Guillermo Ivan. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario; Argentina
Fil: Svetaz, Laura Andrea. Universidad Nacional de Rosario; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Quiroga, Ariel Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; Argentina
Fil: Alvarez, Vera Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Fisiología Experimental. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Fisiología Experimental; Argentina
Fil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina
Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Mar del Plata. Instituto de Investigaciones en Ciencia y Tecnología de Materiales. Universidad Nacional de Mar del Plata. Facultad de Ingeniería. Instituto de Investigaciones en Ciencia y Tecnología de Materiales; Argentina. Universidad Nacional de Rosario; Argentina
description A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients’ comfort and compliance, were considered. Mechanical testing, such as load at break, elongation at break, and mucoadhesive strength were also included as dependent variables. The optimal mucoadhesive film formulation, which should be obtained at a drying temperature of 30 °C, was found to include the combination of CH and HPMC (forming polymers) at 0.25:0.75 ratio, a mixture of polyethylene glycol 400 and propylene glycol as plasticizers (0.07:0.93, 5% w/w), and TCZ loaded at 15 % w/w. The optimal preparation was subjected to exhaustive characterization studies, which revealed that the drug was entrapped in the polymeric matrix in an amorphous state and that the film exhibited a smooth and uniform surface, demonstrating excellent component compatibility. In vitro tests showed that the formulation has an excellent time to kill value (3 min) and lacks cytotoxicity, suggesting that it should be highly effective and safe.
publishDate 2021
dc.date.none.fl_str_mv 2021-10
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/11336/211988
Calvo, Natalia Lorena; Tejada Jacob, Guillermo Ivan; Svetaz, Laura Andrea; Quiroga, Ariel Dario; Alvarez, Vera Alejandra; et al.; Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization; Elsevier Science; Journal of Pharmaceutical and Biomedical Analysis; 205; 10-2021; 1-37
0731-7085
CONICET Digital
CONICET
url http://hdl.handle.net/11336/211988
identifier_str_mv Calvo, Natalia Lorena; Tejada Jacob, Guillermo Ivan; Svetaz, Laura Andrea; Quiroga, Ariel Dario; Alvarez, Vera Alejandra; et al.; Development and optimization of a new tioconazole vaginal mucoadhesive film using an experimental design strategy. Physicochemical and biological characterization; Elsevier Science; Journal of Pharmaceutical and Biomedical Analysis; 205; 10-2021; 1-37
0731-7085
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/S0731708521004143
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jpba.2021.114303
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
application/pdf
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
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score 12.982451

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