Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir

Young women in sub-Saharan Africa have the highest risk of human immunodeficiency virus (HIV) acquisition through sexual contact of all groups. Vaginal controlled release of antiretrovirals is a priority option for the prevention of sexual transmission of the virus in women. In this manuscript, bila...

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Autores: Cazorla-Luna, Raúl, Notario-Pérez, Fernando, Martín-Illana, Araceli, Bedoya, Luis-Miguel, Tamayo Hernando, Aitana, Rubio Alonso, Juan, Ruiz-Caro, Roberto, Veiga, María Dolores
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2020
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/235474
Acceso en línea:http://hdl.handle.net/10261/235474
Access Level:acceso abierto
Palabra clave:In Vitro/Ex Vivo Characterization
Vaginal Mucoadhesive
Ethylcellulose
Biopolymers
Vaginal Sustained Release
Tenofovir
Human Immunodeficiency Virus (HIV)
Prevention
Sexual transmission
Virus
Women
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
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spelling Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of TenofovirCazorla-Luna, RaúlNotario-Pérez, FernandoMartín-Illana, AraceliBedoya, Luis-MiguelTamayo Hernando, AitanaRubio Alonso, JuanRuiz-Caro, RobertoVeiga, María DoloresIn Vitro/Ex Vivo CharacterizationVaginal MucoadhesiveEthylcelluloseBiopolymersVaginal Sustained ReleaseTenofovirHuman Immunodeficiency Virus (HIV)PreventionSexual transmissionVirusWomenhttp://metadata.un.org/sdg/3Ensure healthy lives and promote well-being for all at all agesYoung women in sub-Saharan Africa have the highest risk of human immunodeficiency virus (HIV) acquisition through sexual contact of all groups. Vaginal controlled release of antiretrovirals is a priority option for the prevention of sexual transmission of the virus in women. In this manuscript, bilayer films were prepared based on ethylcellulose and a natural polymer (xanthan or tragacanth gum) plasticized with glycerol and tributylcitrate for tenofovir-controlled release. The mechanical properties and microstructure of the blank films were characterized by texture analysis, Fourier transform infrared spectroscopy, and scanning electron microscopy. The loaded films were evaluated in simulated vaginal fluid through release and swelling studies and ex vivo mucoadhesion assessments. The results show that the preparation method produced bilayer films with adequate mechanical properties. The contribution of both layers allowed the sustained release of tenofovir and a mucoadhesion time of up to 360 h. The toxicity of the materials was evaluated in three cell lines of vaginal origin. The films constituted by ethylcellulose and xanthan gum in a 2:1 proportion (EX2-D) showed the longest mucoadhesion time, with 15 days of tenofovir-controlled release, zero toxicity, and optimal mechanical properties. These films are therefore a promising option for offering women a means of self-protection against the sexual transmission of HIV.This work was supported by project MAT2016-76416-R financed by the Spanish Research Agency and the European Regional Development Fund (AEI/FEDER, UE). R.C.-L. and A.M.-I. are beneficiaries of University Professor Training fellowships granted by the Spanish Ministry of Education, Culture and Sport, and F.N.-P. is the beneficiary of a Research Training Fellowship granted by the Spanish Ministry of Science, Innovation, and Universities.Peer reviewedAmerican Chemical SocietyMinisterio de Economía y Competitividad (España)Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]2021202120202021info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501Postprintinfo:eu-repo/semantics/acceptedVersionhttp://hdl.handle.net/10261/235474reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)Inglés#PLACEHOLDER_PARENT_METADATA_VALUE#info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/MAT2016-76416-Rhttp://dx.doi.org/10.1021/acs.biomac.0c00249Síinfo:eu-repo/semantics/openAccessoai:digital.csic.es:10261/2354742026-05-22T06:33:51Z
dc.title.none.fl_str_mv Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
title Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
spellingShingle Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
Cazorla-Luna, Raúl
In Vitro/Ex Vivo Characterization
Vaginal Mucoadhesive
Ethylcellulose
Biopolymers
Vaginal Sustained Release
Tenofovir
Human Immunodeficiency Virus (HIV)
Prevention
Sexual transmission
Virus
Women
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
title_short Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
title_full Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
title_fullStr Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
title_full_unstemmed Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
title_sort Development and In Vitro/Ex Vivo Characterization of Vaginal Mucoadhesive Bilayer Films Based on Ethylcellulose and Biopolymers for Vaginal Sustained Release of Tenofovir
dc.creator.none.fl_str_mv Cazorla-Luna, Raúl
Notario-Pérez, Fernando
Martín-Illana, Araceli
Bedoya, Luis-Miguel
Tamayo Hernando, Aitana
Rubio Alonso, Juan
Ruiz-Caro, Roberto
Veiga, María Dolores
author Cazorla-Luna, Raúl
author_facet Cazorla-Luna, Raúl
Notario-Pérez, Fernando
Martín-Illana, Araceli
Bedoya, Luis-Miguel
Tamayo Hernando, Aitana
Rubio Alonso, Juan
Ruiz-Caro, Roberto
Veiga, María Dolores
author_role author
author2 Notario-Pérez, Fernando
Martín-Illana, Araceli
Bedoya, Luis-Miguel
Tamayo Hernando, Aitana
Rubio Alonso, Juan
Ruiz-Caro, Roberto
Veiga, María Dolores
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Ministerio de Economía y Competitividad (España)
Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]
dc.subject.none.fl_str_mv In Vitro/Ex Vivo Characterization
Vaginal Mucoadhesive
Ethylcellulose
Biopolymers
Vaginal Sustained Release
Tenofovir
Human Immunodeficiency Virus (HIV)
Prevention
Sexual transmission
Virus
Women
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
topic In Vitro/Ex Vivo Characterization
Vaginal Mucoadhesive
Ethylcellulose
Biopolymers
Vaginal Sustained Release
Tenofovir
Human Immunodeficiency Virus (HIV)
Prevention
Sexual transmission
Virus
Women
http://metadata.un.org/sdg/3
Ensure healthy lives and promote well-being for all at all ages
description Young women in sub-Saharan Africa have the highest risk of human immunodeficiency virus (HIV) acquisition through sexual contact of all groups. Vaginal controlled release of antiretrovirals is a priority option for the prevention of sexual transmission of the virus in women. In this manuscript, bilayer films were prepared based on ethylcellulose and a natural polymer (xanthan or tragacanth gum) plasticized with glycerol and tributylcitrate for tenofovir-controlled release. The mechanical properties and microstructure of the blank films were characterized by texture analysis, Fourier transform infrared spectroscopy, and scanning electron microscopy. The loaded films were evaluated in simulated vaginal fluid through release and swelling studies and ex vivo mucoadhesion assessments. The results show that the preparation method produced bilayer films with adequate mechanical properties. The contribution of both layers allowed the sustained release of tenofovir and a mucoadhesion time of up to 360 h. The toxicity of the materials was evaluated in three cell lines of vaginal origin. The films constituted by ethylcellulose and xanthan gum in a 2:1 proportion (EX2-D) showed the longest mucoadhesion time, with 15 days of tenofovir-controlled release, zero toxicity, and optimal mechanical properties. These films are therefore a promising option for offering women a means of self-protection against the sexual transmission of HIV.
publishDate 2020
dc.date.none.fl_str_mv 2020
2021
2021
2021
dc.type.none.fl_str_mv info:eu-repo/semantics/article
http://purl.org/coar/resource_type/c_6501
Postprint
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10261/235474
url http://hdl.handle.net/10261/235474
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv #PLACEHOLDER_PARENT_METADATA_VALUE#
info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/MAT2016-76416-R
http://dx.doi.org/10.1021/acs.biomac.0c00249
Sí
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv American Chemical Society
publisher.none.fl_str_mv American Chemical Society
dc.source.none.fl_str_mv reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC
instname:Consejo Superior de Investigaciones Científicas (CSIC)
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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