Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs
Autor(a) principal: | |
---|---|
Data de Publicação: | 2019 |
Outros Autores: | , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1208/s12249-019-1439-3 http://hdl.handle.net/11449/190452 |
Resumo: | The vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems. |
id |
UNSP_895f43a10cfe0f135e5fb071081c3a68 |
---|---|
oai_identifier_str |
oai:repositorio.unesp.br:11449/190452 |
network_acronym_str |
UNSP |
network_name_str |
Repositório Institucional da UNESP |
repository_id_str |
2946 |
spelling |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugsdrug delivery systemliquid crystalline systemmucoadhesionnanotechnologyvaginal administrationThe vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems.School of Pharmaceutical Sciences São Paulo State University (UNESP)Paraíba State UniversityCenter for Natural Sciences and Humanities Federal University of ABC (UFABC)School of Pharmaceutical Sciences São Paulo State University (UNESP)Universidade Estadual Paulista (Unesp)Paraíba State UniversityUniversidade Federal do ABC (UFABC)de Araújo, Patricia Rocha [UNESP]Calixto, Giovana Maria Fioramonti [UNESP]da Silva, Isabel Cristiane [UNESP]de Paula Zago, Lucas Henrique [UNESP]Oshiro Junior, João AugustoPavan, Fernando Rogério [UNESP]Ribeiro, Anderson OrzariFontana, Carla Raquel [UNESP]Chorilli, Marlus [UNESP]2019-10-06T17:13:40Z2019-10-06T17:13:40Z2019-08-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1208/s12249-019-1439-3AAPS PharmSciTech, v. 20, n. 6, 2019.1530-9932http://hdl.handle.net/11449/19045210.1208/s12249-019-1439-32-s2.0-85068182314Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengAAPS PharmSciTechinfo:eu-repo/semantics/openAccess2024-06-24T13:46:12Zoai:repositorio.unesp.br:11449/190452Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T21:31:04.458321Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
title |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
spellingShingle |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs de Araújo, Patricia Rocha [UNESP] drug delivery system liquid crystalline system mucoadhesion nanotechnology vaginal administration |
title_short |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
title_full |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
title_fullStr |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
title_full_unstemmed |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
title_sort |
Mucoadhesive In Situ Gelling Liquid Crystalline Precursor System to Improve the Vaginal Administration of Drugs |
author |
de Araújo, Patricia Rocha [UNESP] |
author_facet |
de Araújo, Patricia Rocha [UNESP] Calixto, Giovana Maria Fioramonti [UNESP] da Silva, Isabel Cristiane [UNESP] de Paula Zago, Lucas Henrique [UNESP] Oshiro Junior, João Augusto Pavan, Fernando Rogério [UNESP] Ribeiro, Anderson Orzari Fontana, Carla Raquel [UNESP] Chorilli, Marlus [UNESP] |
author_role |
author |
author2 |
Calixto, Giovana Maria Fioramonti [UNESP] da Silva, Isabel Cristiane [UNESP] de Paula Zago, Lucas Henrique [UNESP] Oshiro Junior, João Augusto Pavan, Fernando Rogério [UNESP] Ribeiro, Anderson Orzari Fontana, Carla Raquel [UNESP] Chorilli, Marlus [UNESP] |
author2_role |
author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Paraíba State University Universidade Federal do ABC (UFABC) |
dc.contributor.author.fl_str_mv |
de Araújo, Patricia Rocha [UNESP] Calixto, Giovana Maria Fioramonti [UNESP] da Silva, Isabel Cristiane [UNESP] de Paula Zago, Lucas Henrique [UNESP] Oshiro Junior, João Augusto Pavan, Fernando Rogério [UNESP] Ribeiro, Anderson Orzari Fontana, Carla Raquel [UNESP] Chorilli, Marlus [UNESP] |
dc.subject.por.fl_str_mv |
drug delivery system liquid crystalline system mucoadhesion nanotechnology vaginal administration |
topic |
drug delivery system liquid crystalline system mucoadhesion nanotechnology vaginal administration |
description |
The vaginal mucosa is a very promising route for drug administration due to its high permeability and the possibility to bypass first pass metabolism; however, current vaginal dosage forms present low retention times due to their dilution in vaginal fluids, which hampers the efficacy of many pharmacological treatments. In order to overcome these problems, this study proposes to develop a mucoadhesive in situ gelling liquid crystalline precursor system composed of 30% of oleic acid and cholesterol (7:1), 40% of ethoxylated and propoxylated cetyl alcohol, and 30% of a dispersion of 16% Poloxamer 407. The effect of the dilution with simulated vaginal fluid (SVF) on this system was evaluated by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), rheological studies, texture profile analysis (TPA), mucoadhesion study, in vitro drug release test using hypericin (HYP) as drug model, and cytotoxicity assay. PLM and SAXS confirmed the formation of an isotropic system. After the addition of three different concentrations of SVF (30, 50, and 100%), the resultant formulations presented anisotropy and characteristics of viscous lamellar phases. Rheology shows that formulations with SVF behaved as a non-Newtonian fluid with suitable shear thinning for vaginal application. TPA and mucoadhesion assays indicated the formation of long-range ordered systems as the amount of SVF increases which may assist in the fixation of the formulation on the vaginal mucosa. The formulations were able to control about 75% of the released HYP demonstrating a sustained release profile. Finally, all formulations acted as safe vaginal drug delivery systems. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-10-06T17:13:40Z 2019-10-06T17:13:40Z 2019-08-01 |
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/10.1208/s12249-019-1439-3 AAPS PharmSciTech, v. 20, n. 6, 2019. 1530-9932 http://hdl.handle.net/11449/190452 10.1208/s12249-019-1439-3 2-s2.0-85068182314 |
url |
http://dx.doi.org/10.1208/s12249-019-1439-3 http://hdl.handle.net/11449/190452 |
identifier_str_mv |
AAPS PharmSciTech, v. 20, n. 6, 2019. 1530-9932 10.1208/s12249-019-1439-3 2-s2.0-85068182314 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
AAPS PharmSciTech |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
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_ |
1808129329466441728 |