Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method

Autores
Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Chiappetta, Diego Andrés; Höcht, Christian; Sosnik, Alejandro Dario; Swai, Hulda
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
AIM: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. MATERIALS & METHODS: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. RESULTS: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. CONCLUSION: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.
Fil: Tshweu, Lesego. Council for Scientific & Industrial Research; Sudáfrica
Fil: Katata, Lebogang. North-West University. Faculty of Agriculture, Science & Technology. Chemistry Department; Sudáfrica. Council for Scientific & Industrial Research; Sudáfrica
Fil: Kalombo, Lonji. Council for Scientific & Industrial Research; Sudáfrica
Fil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Technion - Israel Institute of Technology; Israel
Fil: Swai, Hulda. Council for Scientific & Industrial Research; Sudáfrica
Materia
Hiv
Efavirenz
In Vitro Drug Release
Oral Bioavailability
Poly (Epsilon-Caprolactone)
Spray Drying
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/15949
Acceder
id CONICETDig_88b8ec4edba3244f5ebc9866b763e9e6
oai_identifier_str oai:ri.conicet.gov.ar:11336/15949
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying methodTshweu, LesegoKatata, LebogangKalombo, LonjiChiappetta, Diego AndrésHöcht, ChristianSosnik, Alejandro DarioSwai, HuldaHivEfavirenzIn Vitro Drug ReleaseOral BioavailabilityPoly (Epsilon-Caprolactone)Spray Dryinghttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2AIM: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. MATERIALS & METHODS: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. RESULTS: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. CONCLUSION: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.Fil: Tshweu, Lesego. Council for Scientific & Industrial Research; SudáfricaFil: Katata, Lebogang. North-West University. Faculty of Agriculture, Science & Technology. Chemistry Department; Sudáfrica. Council for Scientific & Industrial Research; SudáfricaFil: Kalombo, Lonji. Council for Scientific & Industrial Research; SudáfricaFil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Technion - Israel Institute of Technology; IsraelFil: Swai, Hulda. Council for Scientific & Industrial Research; SudáfricaFuture Medicine2014-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/15949Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Chiappetta, Diego Andrés; Höcht, Christian; et al.; Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method; Future Medicine; Nanomedicine; 9; 12; 11-2014; 1821-18331743-5889enginfo:eu-repo/semantics/altIdentifier/url/http://www.futuremedicine.com/doi/10.2217/nnm.13.167info:eu-repo/semantics/altIdentifier/doi/10.2217/nnm.13.167info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:06:08Zoai:ri.conicet.gov.ar:11336/15949instacron: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 10:06:08.806CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
title Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
spellingShingle Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
Tshweu, Lesego
Hiv
Efavirenz
In Vitro Drug Release
Oral Bioavailability
Poly (Epsilon-Caprolactone)
Spray Drying
title_short Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
title_full Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
title_fullStr Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
title_full_unstemmed Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
title_sort Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method
dc.creator.none.fl_str_mv Tshweu, Lesego
Katata, Lebogang
Kalombo, Lonji
Chiappetta, Diego Andrés
Höcht, Christian
Sosnik, Alejandro Dario
Swai, Hulda
author Tshweu, Lesego
author_facet Tshweu, Lesego
Katata, Lebogang
Kalombo, Lonji
Chiappetta, Diego Andrés
Höcht, Christian
Sosnik, Alejandro Dario
Swai, Hulda
author_role author
author2 Katata, Lebogang
Kalombo, Lonji
Chiappetta, Diego Andrés
Höcht, Christian
Sosnik, Alejandro Dario
Swai, Hulda
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Hiv
Efavirenz
In Vitro Drug Release
Oral Bioavailability
Poly (Epsilon-Caprolactone)
Spray Drying
topic Hiv
Efavirenz
In Vitro Drug Release
Oral Bioavailability
Poly (Epsilon-Caprolactone)
Spray Drying
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv AIM: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. MATERIALS & METHODS: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. RESULTS: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. CONCLUSION: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.
Fil: Tshweu, Lesego. Council for Scientific & Industrial Research; Sudáfrica
Fil: Katata, Lebogang. North-West University. Faculty of Agriculture, Science & Technology. Chemistry Department; Sudáfrica. Council for Scientific & Industrial Research; Sudáfrica
Fil: Kalombo, Lonji. Council for Scientific & Industrial Research; Sudáfrica
Fil: Chiappetta, Diego Andrés. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina. Technion - Israel Institute of Technology; Israel
Fil: Swai, Hulda. Council for Scientific & Industrial Research; Sudáfrica
description AIM: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. MATERIALS & METHODS: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. RESULTS: NPs displayed a hydrodynamic diameter of 200-250 nm. The encapsulation efficiency was 86-93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. CONCLUSION: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.
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/11336/15949
Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Chiappetta, Diego Andrés; Höcht, Christian; et al.; Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method; Future Medicine; Nanomedicine; 9; 12; 11-2014; 1821-1833
1743-5889
url http://hdl.handle.net/11336/15949
identifier_str_mv Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Chiappetta, Diego Andrés; Höcht, Christian; et al.; Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method; Future Medicine; Nanomedicine; 9; 12; 11-2014; 1821-1833
1743-5889
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.futuremedicine.com/doi/10.2217/nnm.13.167
info:eu-repo/semantics/altIdentifier/doi/10.2217/nnm.13.167
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Future Medicine
publisher.none.fl_str_mv Future Medicine
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_ 1844613906732941312
score 13.070432

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