Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability

Autores
Seremeta, Katia Pamela; Reyes Tur, María I.; Martínez Pérez, Sandra; Höcht, Christian; Taira, Carlos Alberto; López Hernández, Orestes D.; Sosnik, Alejandro Dario
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Didanosine (ddI) is a water-soluble antiretroviral used in the treatment of HIV that undergoes fast gastric degradation to an inactive hypoxanthine. Therefore, its oral bioavailability is relatively low (20–40%). In this work, we investigated for the first time a scalable open-loop spray-drying method with co-current flow for the encapsulation of ddI (model drug) within particles of the biocompatible polyester poly(epsilon-caprolactone). The average diameter of the particles was 36–118 μm and the morphology spherical. The encapsulation efficiency ranged from 60% to 100% with yields of up to 65%. ATR/FT-IR analysis indicated that most of the drug was encapsulated within the particles. In vitro release assays showed that the particles released the drug within 120 min. Finally, oral administration to rats led to a statistically significant 2.5-fold increase of the bioavailability with respect to a ddI aqueous solution, highlighting the potential of this technology to encapsulate efficiently other hydrophilic antiretrovirals and, by doing so, to overcome different biopharmaceutical drawbacks associated with the oral administration.
Fil: Seremeta, Katia Pamela. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Reyes Tur, María I.. AICA Laboratories; Cuba
Fil: Martínez Pérez, Sandra. LIORAD Laboratories; Cuba
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: López Hernández, Orestes D.. Ambato Technical University. Faculty of Food Science and Engineering; Ecuador
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Technion - Israel Institute of Technology; Israel
Materia
Hiv Therapy
Didanosine
Poly (Epsilon-Caprolactone) Microparticles
Spray-Drying
Enhanced Oral Bioavailability
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/15783
Acceder
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network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailabilitySeremeta, Katia PamelaReyes Tur, María I.Martínez Pérez, SandraHöcht, ChristianTaira, Carlos AlbertoLópez Hernández, Orestes D.Sosnik, Alejandro DarioHiv TherapyDidanosinePoly (Epsilon-Caprolactone) MicroparticlesSpray-DryingEnhanced Oral Bioavailabilityhttps://purl.org/becyt/ford/3.3https://purl.org/becyt/ford/3Didanosine (ddI) is a water-soluble antiretroviral used in the treatment of HIV that undergoes fast gastric degradation to an inactive hypoxanthine. Therefore, its oral bioavailability is relatively low (20–40%). In this work, we investigated for the first time a scalable open-loop spray-drying method with co-current flow for the encapsulation of ddI (model drug) within particles of the biocompatible polyester poly(epsilon-caprolactone). The average diameter of the particles was 36–118 μm and the morphology spherical. The encapsulation efficiency ranged from 60% to 100% with yields of up to 65%. ATR/FT-IR analysis indicated that most of the drug was encapsulated within the particles. In vitro release assays showed that the particles released the drug within 120 min. Finally, oral administration to rats led to a statistically significant 2.5-fold increase of the bioavailability with respect to a ddI aqueous solution, highlighting the potential of this technology to encapsulate efficiently other hydrophilic antiretrovirals and, by doing so, to overcome different biopharmaceutical drawbacks associated with the oral administration.Fil: Seremeta, Katia Pamela. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Reyes Tur, María I.. AICA Laboratories; CubaFil: Martínez Pérez, Sandra. LIORAD Laboratories; CubaFil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Taira, Carlos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: López Hernández, Orestes D.. Ambato Technical University. Faculty of Food Science and Engineering; EcuadorFil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Technion - Israel Institute of Technology; IsraelElsevier Science2014-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/15783Seremeta, Katia Pamela; Reyes Tur, María I.; Martínez Pérez, Sandra; Höcht, Christian; Taira, Carlos Alberto; et al.; Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 123; 11-2014; 515-5230927-7765enginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.colsurfb.2014.09.055info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0927776514005268info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:46:31Zoai:ri.conicet.gov.ar:11336/15783instacron: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:34982025-09-03 09:46:31.342CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
title Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
spellingShingle Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
Seremeta, Katia Pamela
Hiv Therapy
Didanosine
Poly (Epsilon-Caprolactone) Microparticles
Spray-Drying
Enhanced Oral Bioavailability
title_short Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
title_full Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
title_fullStr Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
title_full_unstemmed Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
title_sort Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability
dc.creator.none.fl_str_mv Seremeta, Katia Pamela
Reyes Tur, María I.
Martínez Pérez, Sandra
Höcht, Christian
Taira, Carlos Alberto
López Hernández, Orestes D.
Sosnik, Alejandro Dario
author Seremeta, Katia Pamela
author_facet Seremeta, Katia Pamela
Reyes Tur, María I.
Martínez Pérez, Sandra
Höcht, Christian
Taira, Carlos Alberto
López Hernández, Orestes D.
Sosnik, Alejandro Dario
author_role author
author2 Reyes Tur, María I.
Martínez Pérez, Sandra
Höcht, Christian
Taira, Carlos Alberto
López Hernández, Orestes D.
Sosnik, Alejandro Dario
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Hiv Therapy
Didanosine
Poly (Epsilon-Caprolactone) Microparticles
Spray-Drying
Enhanced Oral Bioavailability
topic Hiv Therapy
Didanosine
Poly (Epsilon-Caprolactone) Microparticles
Spray-Drying
Enhanced Oral Bioavailability
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.3
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv Didanosine (ddI) is a water-soluble antiretroviral used in the treatment of HIV that undergoes fast gastric degradation to an inactive hypoxanthine. Therefore, its oral bioavailability is relatively low (20–40%). In this work, we investigated for the first time a scalable open-loop spray-drying method with co-current flow for the encapsulation of ddI (model drug) within particles of the biocompatible polyester poly(epsilon-caprolactone). The average diameter of the particles was 36–118 μm and the morphology spherical. The encapsulation efficiency ranged from 60% to 100% with yields of up to 65%. ATR/FT-IR analysis indicated that most of the drug was encapsulated within the particles. In vitro release assays showed that the particles released the drug within 120 min. Finally, oral administration to rats led to a statistically significant 2.5-fold increase of the bioavailability with respect to a ddI aqueous solution, highlighting the potential of this technology to encapsulate efficiently other hydrophilic antiretrovirals and, by doing so, to overcome different biopharmaceutical drawbacks associated with the oral administration.
Fil: Seremeta, Katia Pamela. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Reyes Tur, María I.. AICA Laboratories; Cuba
Fil: Martínez Pérez, Sandra. LIORAD Laboratories; Cuba
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: López Hernández, Orestes D.. Ambato Technical University. Faculty of Food Science and Engineering; Ecuador
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Technion - Israel Institute of Technology; Israel
description Didanosine (ddI) is a water-soluble antiretroviral used in the treatment of HIV that undergoes fast gastric degradation to an inactive hypoxanthine. Therefore, its oral bioavailability is relatively low (20–40%). In this work, we investigated for the first time a scalable open-loop spray-drying method with co-current flow for the encapsulation of ddI (model drug) within particles of the biocompatible polyester poly(epsilon-caprolactone). The average diameter of the particles was 36–118 μm and the morphology spherical. The encapsulation efficiency ranged from 60% to 100% with yields of up to 65%. ATR/FT-IR analysis indicated that most of the drug was encapsulated within the particles. In vitro release assays showed that the particles released the drug within 120 min. Finally, oral administration to rats led to a statistically significant 2.5-fold increase of the bioavailability with respect to a ddI aqueous solution, highlighting the potential of this technology to encapsulate efficiently other hydrophilic antiretrovirals and, by doing so, to overcome different biopharmaceutical drawbacks associated with the oral administration.
publishDate 2014
dc.date.none.fl_str_mv 2014-11
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/11336/15783
Seremeta, Katia Pamela; Reyes Tur, María I.; Martínez Pérez, Sandra; Höcht, Christian; Taira, Carlos Alberto; et al.; Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 123; 11-2014; 515-523
0927-7765
url http://hdl.handle.net/11336/15783
identifier_str_mv Seremeta, Katia Pamela; Reyes Tur, María I.; Martínez Pérez, Sandra; Höcht, Christian; Taira, Carlos Alberto; et al.; Spray-dried didanosine-loaded polymeric particles for enhanced oral bioavailability; Elsevier Science; Colloids and Surfaces B: Biointerfaces; 123; 11-2014; 515-523
0927-7765
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.colsurfb.2014.09.055
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0927776514005268
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv 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
_version_ 1842268800093782016
score 13.13397

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