Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine
Autor(a) principal: | |
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Data de Publicação: | 2022 |
Outros Autores: | , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1080/10837450.2022.2097258 http://hdl.handle.net/11449/242045 |
Resumo: | Zidovudine (AZT) has been widely used alone or in combination with other antiretroviral drugs for the treatment of human immunodeficiency virus. Its erratic oral bioavailability necessitates frequent administration of high doses, resulting in severe side effects. In this study, the design of mucoadhesive solid dispersions (SDs) based on chitosan (CS) and hypromellose phthalate (HP) was rationalized as a potential approach to modulate AZT physicochemical and pharmaceutical properties. SDs were prepared at different drug:polymer ratios, using an eco-friendly technique, which avoids the use of organic solvents. Particles with diameter from 56 to 73 µm and negative zeta potentials (–27 to −32 mV) were successfully prepared, achieving high drug content. Infrared spectroscopy revealed interactions between polymers but no interactions between the polymers and AZT. Calorimetry and X-ray diffraction analyses showed that AZT was amorphized into the SDs. The mucoadhesive properties of SDs were evidenced, and the control of AZT release rates from the matrix was achieved, mainly in acid media. The simple, low-cost, and scalable technology proposed for production of SDs as a carrier platform for AZT is an innovative approach, and it proved to be a feasible strategy for modulation the physico-chemical, mucoadhesive, and release properties of the drug. |
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Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudinechitosancontrolled releasemucoadhesionoral deliverySolid dispersionZidovudine (AZT) has been widely used alone or in combination with other antiretroviral drugs for the treatment of human immunodeficiency virus. Its erratic oral bioavailability necessitates frequent administration of high doses, resulting in severe side effects. In this study, the design of mucoadhesive solid dispersions (SDs) based on chitosan (CS) and hypromellose phthalate (HP) was rationalized as a potential approach to modulate AZT physicochemical and pharmaceutical properties. SDs were prepared at different drug:polymer ratios, using an eco-friendly technique, which avoids the use of organic solvents. Particles with diameter from 56 to 73 µm and negative zeta potentials (–27 to −32 mV) were successfully prepared, achieving high drug content. Infrared spectroscopy revealed interactions between polymers but no interactions between the polymers and AZT. Calorimetry and X-ray diffraction analyses showed that AZT was amorphized into the SDs. The mucoadhesive properties of SDs were evidenced, and the control of AZT release rates from the matrix was achieved, mainly in acid media. The simple, low-cost, and scalable technology proposed for production of SDs as a carrier platform for AZT is an innovative approach, and it proved to be a feasible strategy for modulation the physico-chemical, mucoadhesive, and release properties of the drug.School of Pharmaceutical Sciences São Paulo State University (UNESP)School of Pharmaceutical Sciences São Paulo State University (UNESP)Universidade Estadual Paulista (UNESP)Pedreiro, Liliane Neves [UNESP]Boni, Fernanda Isadora [UNESP]Cury, Beatriz Stringhetti Ferreira [UNESP]Ferreira, Natália Noronha [UNESP]Gremião, Maria Palmira Daflon [UNESP]2023-03-02T08:17:54Z2023-03-02T08:17:54Z2022-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article615-624http://dx.doi.org/10.1080/10837450.2022.2097258Pharmaceutical Development and Technology, v. 27, n. 5, p. 615-624, 2022.1097-98671083-7450http://hdl.handle.net/11449/24204510.1080/10837450.2022.20972582-s2.0-85134301382Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengPharmaceutical Development and Technologyinfo:eu-repo/semantics/openAccess2024-06-24T13:46:34Zoai:repositorio.unesp.br:11449/242045Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T23:51:53.907385Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
title |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
spellingShingle |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine Pedreiro, Liliane Neves [UNESP] chitosan controlled release mucoadhesion oral delivery Solid dispersion |
title_short |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
title_full |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
title_fullStr |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
title_full_unstemmed |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
title_sort |
Solid dispersions based on chitosan/hypromellose phthalate blends to modulate pharmaceutical properties of zidovudine |
author |
Pedreiro, Liliane Neves [UNESP] |
author_facet |
Pedreiro, Liliane Neves [UNESP] Boni, Fernanda Isadora [UNESP] Cury, Beatriz Stringhetti Ferreira [UNESP] Ferreira, Natália Noronha [UNESP] Gremião, Maria Palmira Daflon [UNESP] |
author_role |
author |
author2 |
Boni, Fernanda Isadora [UNESP] Cury, Beatriz Stringhetti Ferreira [UNESP] Ferreira, Natália Noronha [UNESP] Gremião, Maria Palmira Daflon [UNESP] |
author2_role |
author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (UNESP) |
dc.contributor.author.fl_str_mv |
Pedreiro, Liliane Neves [UNESP] Boni, Fernanda Isadora [UNESP] Cury, Beatriz Stringhetti Ferreira [UNESP] Ferreira, Natália Noronha [UNESP] Gremião, Maria Palmira Daflon [UNESP] |
dc.subject.por.fl_str_mv |
chitosan controlled release mucoadhesion oral delivery Solid dispersion |
topic |
chitosan controlled release mucoadhesion oral delivery Solid dispersion |
description |
Zidovudine (AZT) has been widely used alone or in combination with other antiretroviral drugs for the treatment of human immunodeficiency virus. Its erratic oral bioavailability necessitates frequent administration of high doses, resulting in severe side effects. In this study, the design of mucoadhesive solid dispersions (SDs) based on chitosan (CS) and hypromellose phthalate (HP) was rationalized as a potential approach to modulate AZT physicochemical and pharmaceutical properties. SDs were prepared at different drug:polymer ratios, using an eco-friendly technique, which avoids the use of organic solvents. Particles with diameter from 56 to 73 µm and negative zeta potentials (–27 to −32 mV) were successfully prepared, achieving high drug content. Infrared spectroscopy revealed interactions between polymers but no interactions between the polymers and AZT. Calorimetry and X-ray diffraction analyses showed that AZT was amorphized into the SDs. The mucoadhesive properties of SDs were evidenced, and the control of AZT release rates from the matrix was achieved, mainly in acid media. The simple, low-cost, and scalable technology proposed for production of SDs as a carrier platform for AZT is an innovative approach, and it proved to be a feasible strategy for modulation the physico-chemical, mucoadhesive, and release properties of the drug. |
publishDate |
2022 |
dc.date.none.fl_str_mv |
2022-01-01 2023-03-02T08:17:54Z 2023-03-02T08:17:54Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1080/10837450.2022.2097258 Pharmaceutical Development and Technology, v. 27, n. 5, p. 615-624, 2022. 1097-9867 1083-7450 http://hdl.handle.net/11449/242045 10.1080/10837450.2022.2097258 2-s2.0-85134301382 |
url |
http://dx.doi.org/10.1080/10837450.2022.2097258 http://hdl.handle.net/11449/242045 |
identifier_str_mv |
Pharmaceutical Development and Technology, v. 27, n. 5, p. 615-624, 2022. 1097-9867 1083-7450 10.1080/10837450.2022.2097258 2-s2.0-85134301382 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Pharmaceutical Development and Technology |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
615-624 |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129559511433216 |