New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance

Autores
Costa, Rogeria Nunes; Reviglio, Ana Lucía; Siedler, Sana; Cardoso, Simone G.; Garro Linck, Yamila; Monti, Gustavo Alberto; Carvalho, Alexandre Magnus G.; Resende, Jackson A. L. C.; Chaves, Marcelo H. C.; Rocha, Helvético Vinícius Antunes; Choquesillo Lazarte, Duane; Infantes, Lourdes; Cuffini, Silvia Lucia
Año de publicación
2020
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In the pharmaceutical area, some drugs exhibit physicochemical properties that adversely affect the formulation processes for bioavailability and effectiveness. Nevirapine (NVP) is an antiretroviral drug that presents low aqueous solubility, which directly impacts its bioavailability. Among all possible modifications, multicomponent crystals, such as cocrystals and eutectic compositions, have been successfully used to improve the solubility of drugs. In this work, the propensity of the formation of multicomponent systems of NVP with seven possible coformers were predicted and tested: salicylic acid (SA), 3-hydroxybenzoic acid (3HBZC), 4-hydroxybenzoic acid (4HBZC), saccharin (SAC), theophylline (THEO), caffeine (CAF), and urea (URE). Results indicate that NVP-SA, NVP-SAC, NVP-3HBZC, and NVP-4HBZC are cocrystals, whereas NVP-THEO and NVP-CAF are eutectic materials, and NVP-URE is a solid physical mixture. A temperature-dependent disorder behavior was identified for NVP-SA cocrystal. Dissolution studies for the eutectic materials are reported, evidencing that these materials exhibit a significant increase in NVP dissolution kinetics.
Fil: Costa, Rogeria Nunes. Universidade Federal de Sao Paulo; Brasil
Fil: Reviglio, Ana Lucía. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Siedler, Sana. Universidade Federal de Santa Catarina; Brasil
Fil: Cardoso, Simone G.. Universidade Federal de Santa Catarina; Brasil
Fil: Garro Linck, Yamila. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Carvalho, Alexandre Magnus G.. Centro Nacional de Pesquisa em Energia e Materiais; Brasil
Fil: Resende, Jackson A. L. C.. Universidade Federal do Mato Grosso do Sul; Brasil
Fil: Chaves, Marcelo H. C.. Fundación Oswaldo Cruz; Brasil
Fil: Rocha, Helvético Vinícius Antunes. Fundación Oswaldo Cruz; Brasil
Fil: Choquesillo Lazarte, Duane. Consejo Superior de Investigaciones Científicas; España. Universidad de Granada; España
Fil: Infantes, Lourdes. Consejo Superior de Investigaciones Científicas; España. Instituto de Química Física Rocasolano; España
Fil: Cuffini, Silvia Lucia. Universidade de Sao Paulo; Brasil
Materia
NEVIRAPINE
COCRYSTAL
EUTECTICS
DISSOLUTION IMPROVEMENT
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:11336/124421
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/124421
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution PerformanceCosta, Rogeria NunesReviglio, Ana LucíaSiedler, SanaCardoso, Simone G.Garro Linck, YamilaMonti, Gustavo AlbertoCarvalho, Alexandre Magnus G.Resende, Jackson A. L. C.Chaves, Marcelo H. C.Rocha, Helvético Vinícius AntunesChoquesillo Lazarte, DuaneInfantes, LourdesCuffini, Silvia LuciaNEVIRAPINECOCRYSTALEUTECTICSDISSOLUTION IMPROVEMENThttps://purl.org/becyt/ford/1.3https://purl.org/becyt/ford/1In the pharmaceutical area, some drugs exhibit physicochemical properties that adversely affect the formulation processes for bioavailability and effectiveness. Nevirapine (NVP) is an antiretroviral drug that presents low aqueous solubility, which directly impacts its bioavailability. Among all possible modifications, multicomponent crystals, such as cocrystals and eutectic compositions, have been successfully used to improve the solubility of drugs. In this work, the propensity of the formation of multicomponent systems of NVP with seven possible coformers were predicted and tested: salicylic acid (SA), 3-hydroxybenzoic acid (3HBZC), 4-hydroxybenzoic acid (4HBZC), saccharin (SAC), theophylline (THEO), caffeine (CAF), and urea (URE). Results indicate that NVP-SA, NVP-SAC, NVP-3HBZC, and NVP-4HBZC are cocrystals, whereas NVP-THEO and NVP-CAF are eutectic materials, and NVP-URE is a solid physical mixture. A temperature-dependent disorder behavior was identified for NVP-SA cocrystal. Dissolution studies for the eutectic materials are reported, evidencing that these materials exhibit a significant increase in NVP dissolution kinetics.Fil: Costa, Rogeria Nunes. Universidade Federal de Sao Paulo; BrasilFil: Reviglio, Ana Lucía. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; ArgentinaFil: Siedler, Sana. Universidade Federal de Santa Catarina; BrasilFil: Cardoso, Simone G.. Universidade Federal de Santa Catarina; BrasilFil: Garro Linck, Yamila. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; ArgentinaFil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; ArgentinaFil: Carvalho, Alexandre Magnus G.. Centro Nacional de Pesquisa em Energia e Materiais; BrasilFil: Resende, Jackson A. L. C.. Universidade Federal do Mato Grosso do Sul; BrasilFil: Chaves, Marcelo H. C.. Fundación Oswaldo Cruz; BrasilFil: Rocha, Helvético Vinícius Antunes. Fundación Oswaldo Cruz; BrasilFil: Choquesillo Lazarte, Duane. Consejo Superior de Investigaciones Científicas; España. Universidad de Granada; EspañaFil: Infantes, Lourdes. Consejo Superior de Investigaciones Científicas; España. Instituto de Química Física Rocasolano; EspañaFil: Cuffini, Silvia Lucia. Universidade de Sao Paulo; BrasilAmerican Chemical Society2020-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/124421Costa, Rogeria Nunes; Reviglio, Ana Lucía; Siedler, Sana; Cardoso, Simone G.; Garro Linck, Yamila; et al.; New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance; American Chemical Society; Crystal Growth & Design; 20; 2; 2-2020; 688-6981528-7483CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/acs.cgd.9b01129info:eu-repo/semantics/altIdentifier/doi/10.1021/acs.cgd.9b01129info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:46:25Zoai:ri.conicet.gov.ar:11336/124421instacron: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:34982025-09-29 10:46:25.92CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
title New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
spellingShingle New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
Costa, Rogeria Nunes
NEVIRAPINE
COCRYSTAL
EUTECTICS
DISSOLUTION IMPROVEMENT
title_short New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
title_full New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
title_fullStr New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
title_full_unstemmed New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
title_sort New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance
dc.creator.none.fl_str_mv Costa, Rogeria Nunes
Reviglio, Ana Lucía
Siedler, Sana
Cardoso, Simone G.
Garro Linck, Yamila
Monti, Gustavo Alberto
Carvalho, Alexandre Magnus G.
Resende, Jackson A. L. C.
Chaves, Marcelo H. C.
Rocha, Helvético Vinícius Antunes
Choquesillo Lazarte, Duane
Infantes, Lourdes
Cuffini, Silvia Lucia
author Costa, Rogeria Nunes
author_facet Costa, Rogeria Nunes
Reviglio, Ana Lucía
Siedler, Sana
Cardoso, Simone G.
Garro Linck, Yamila
Monti, Gustavo Alberto
Carvalho, Alexandre Magnus G.
Resende, Jackson A. L. C.
Chaves, Marcelo H. C.
Rocha, Helvético Vinícius Antunes
Choquesillo Lazarte, Duane
Infantes, Lourdes
Cuffini, Silvia Lucia
author_role author
author2 Reviglio, Ana Lucía
Siedler, Sana
Cardoso, Simone G.
Garro Linck, Yamila
Monti, Gustavo Alberto
Carvalho, Alexandre Magnus G.
Resende, Jackson A. L. C.
Chaves, Marcelo H. C.
Rocha, Helvético Vinícius Antunes
Choquesillo Lazarte, Duane
Infantes, Lourdes
Cuffini, Silvia Lucia
author2_role author
author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv NEVIRAPINE
COCRYSTAL
EUTECTICS
DISSOLUTION IMPROVEMENT
topic NEVIRAPINE
COCRYSTAL
EUTECTICS
DISSOLUTION IMPROVEMENT
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.3
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv In the pharmaceutical area, some drugs exhibit physicochemical properties that adversely affect the formulation processes for bioavailability and effectiveness. Nevirapine (NVP) is an antiretroviral drug that presents low aqueous solubility, which directly impacts its bioavailability. Among all possible modifications, multicomponent crystals, such as cocrystals and eutectic compositions, have been successfully used to improve the solubility of drugs. In this work, the propensity of the formation of multicomponent systems of NVP with seven possible coformers were predicted and tested: salicylic acid (SA), 3-hydroxybenzoic acid (3HBZC), 4-hydroxybenzoic acid (4HBZC), saccharin (SAC), theophylline (THEO), caffeine (CAF), and urea (URE). Results indicate that NVP-SA, NVP-SAC, NVP-3HBZC, and NVP-4HBZC are cocrystals, whereas NVP-THEO and NVP-CAF are eutectic materials, and NVP-URE is a solid physical mixture. A temperature-dependent disorder behavior was identified for NVP-SA cocrystal. Dissolution studies for the eutectic materials are reported, evidencing that these materials exhibit a significant increase in NVP dissolution kinetics.
Fil: Costa, Rogeria Nunes. Universidade Federal de Sao Paulo; Brasil
Fil: Reviglio, Ana Lucía. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Siedler, Sana. Universidade Federal de Santa Catarina; Brasil
Fil: Cardoso, Simone G.. Universidade Federal de Santa Catarina; Brasil
Fil: Garro Linck, Yamila. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Monti, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Física Enrique Gaviola. Universidad Nacional de Córdoba. Instituto de Física Enrique Gaviola; Argentina. Universidad Nacional de Córdoba. Facultad de Matemática, Astronomía y Física; Argentina
Fil: Carvalho, Alexandre Magnus G.. Centro Nacional de Pesquisa em Energia e Materiais; Brasil
Fil: Resende, Jackson A. L. C.. Universidade Federal do Mato Grosso do Sul; Brasil
Fil: Chaves, Marcelo H. C.. Fundación Oswaldo Cruz; Brasil
Fil: Rocha, Helvético Vinícius Antunes. Fundación Oswaldo Cruz; Brasil
Fil: Choquesillo Lazarte, Duane. Consejo Superior de Investigaciones Científicas; España. Universidad de Granada; España
Fil: Infantes, Lourdes. Consejo Superior de Investigaciones Científicas; España. Instituto de Química Física Rocasolano; España
Fil: Cuffini, Silvia Lucia. Universidade de Sao Paulo; Brasil
description In the pharmaceutical area, some drugs exhibit physicochemical properties that adversely affect the formulation processes for bioavailability and effectiveness. Nevirapine (NVP) is an antiretroviral drug that presents low aqueous solubility, which directly impacts its bioavailability. Among all possible modifications, multicomponent crystals, such as cocrystals and eutectic compositions, have been successfully used to improve the solubility of drugs. In this work, the propensity of the formation of multicomponent systems of NVP with seven possible coformers were predicted and tested: salicylic acid (SA), 3-hydroxybenzoic acid (3HBZC), 4-hydroxybenzoic acid (4HBZC), saccharin (SAC), theophylline (THEO), caffeine (CAF), and urea (URE). Results indicate that NVP-SA, NVP-SAC, NVP-3HBZC, and NVP-4HBZC are cocrystals, whereas NVP-THEO and NVP-CAF are eutectic materials, and NVP-URE is a solid physical mixture. A temperature-dependent disorder behavior was identified for NVP-SA cocrystal. Dissolution studies for the eutectic materials are reported, evidencing that these materials exhibit a significant increase in NVP dissolution kinetics.
publishDate 2020
dc.date.none.fl_str_mv 2020-02
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/11336/124421
Costa, Rogeria Nunes; Reviglio, Ana Lucía; Siedler, Sana; Cardoso, Simone G.; Garro Linck, Yamila; et al.; New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance; American Chemical Society; Crystal Growth & Design; 20; 2; 2-2020; 688-698
1528-7483
CONICET Digital
CONICET
url http://hdl.handle.net/11336/124421
identifier_str_mv Costa, Rogeria Nunes; Reviglio, Ana Lucía; Siedler, Sana; Cardoso, Simone G.; Garro Linck, Yamila; et al.; New Multicomponent Forms of the Antiretroviral Nevirapine with Improved Dissolution Performance; American Chemical Society; Crystal Growth & Design; 20; 2; 2-2020; 688-698
1528-7483
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://pubs.acs.org/doi/10.1021/acs.cgd.9b01129
info:eu-repo/semantics/altIdentifier/doi/10.1021/acs.cgd.9b01129
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 American Chemical Society
publisher.none.fl_str_mv American Chemical Society
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 13.070432

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