Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV

Autores
Chiappetta, Diego Andrés; Hocht, Christian; Opezzo, Javier A. W.; Sosnik, Alejandro Dario
Año de publicación
2012
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
We investigated the intranasal administration of poly(ethylene oxide)–poly(propylene oxide) polymeric micelles loaded with high payloads of the first-line antiretroviral drug efavirenz for targeting to the CNS. The effect of micellar size and composition and drug payload was assessed, employing simple micelles made of a highly hydrophilic copolymer, poloxamer F127, loaded with 20 mg/ml drug and mixed micelles containing 75% of a medium hydrophobic poloxamine, T904, and 25% F127 loaded with 20 and 30 mg/ml drug, respectively. F127 confers high physical stability, while T904 substantially improves the encapsulation capacity of the micelles. The bioavailability of the drug in the CNS was increased fourfold and the relative exposure index (ratio between the area-under-the-curve in the CNS and plasma) was increased fivefold with respect to the same system administered intravenously. These findings demonstrate the potential of this scalable and cost-viable strategy to attack the HIV sanctuary in the CNS.
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. Oficina de Coordinación Administrativa Houssay; Argentina;
Fil: Hocht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;
Fil: Opezzo, Javier A. W.. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;
Fil: Sosnik, Alejandro Dario. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina;
Materia
Anatomical Targeting To the Brain
Cns
Efavirenz-Loaded Micelles
Hiv Reservoirs
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:11336/1865
Acceder
id CONICETDig_259fc86d60d5ded2d0dff46e21a59074
oai_identifier_str oai:ri.conicet.gov.ar:11336/1865
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIVChiappetta, Diego AndrésHocht, ChristianOpezzo, Javier A. W.Sosnik, Alejandro DarioAnatomical Targeting To the BrainCnsEfavirenz-Loaded MicellesHiv Reservoirshttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2https://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3We investigated the intranasal administration of poly(ethylene oxide)–poly(propylene oxide) polymeric micelles loaded with high payloads of the first-line antiretroviral drug efavirenz for targeting to the CNS. The effect of micellar size and composition and drug payload was assessed, employing simple micelles made of a highly hydrophilic copolymer, poloxamer F127, loaded with 20 mg/ml drug and mixed micelles containing 75% of a medium hydrophobic poloxamine, T904, and 25% F127 loaded with 20 and 30 mg/ml drug, respectively. F127 confers high physical stability, while T904 substantially improves the encapsulation capacity of the micelles. The bioavailability of the drug in the CNS was increased fourfold and the relative exposure index (ratio between the area-under-the-curve in the CNS and plasma) was increased fivefold with respect to the same system administered intravenously. These findings demonstrate the potential of this scalable and cost-viable strategy to attack the HIV sanctuary in the CNS.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. Oficina de Coordinación Administrativa Houssay; Argentina;Fil: Hocht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;Fil: Opezzo, Javier A. W.. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;Fil: Sosnik, Alejandro Dario. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina;Future Medicine2012-11-22info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/1865Chiappetta, Diego Andrés; Hocht, Christian; Opezzo, Javier A. W.; Sosnik, Alejandro Dario; Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV; Future Medicine; Nanomedicine; 8; 2; 22-11-2012; 223-2371743-5889enginfo:eu-repo/semantics/altIdentifier/doi/DOI:10.2217/nnm.12.104info:eu-repo/semantics/altIdentifier/url/http://www.futuremedicine.com/doi/abs/10.2217/nnm.12.104?url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&rfr_dat=cr_pub%3Dpubmed&info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T14:26:19Zoai:ri.conicet.gov.ar:11336/1865instacron: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:34982025-10-15 14:26:20.18CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
title Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
spellingShingle Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
Chiappetta, Diego Andrés
Anatomical Targeting To the Brain
Cns
Efavirenz-Loaded Micelles
Hiv Reservoirs
title_short Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
title_full Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
title_fullStr Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
title_full_unstemmed Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
title_sort Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV
dc.creator.none.fl_str_mv Chiappetta, Diego Andrés
Hocht, Christian
Opezzo, Javier A. W.
Sosnik, Alejandro Dario
author Chiappetta, Diego Andrés
author_facet Chiappetta, Diego Andrés
Hocht, Christian
Opezzo, Javier A. W.
Sosnik, Alejandro Dario
author_role author
author2 Hocht, Christian
Opezzo, Javier A. W.
Sosnik, Alejandro Dario
author2_role author
author
author
dc.subject.none.fl_str_mv Anatomical Targeting To the Brain
Cns
Efavirenz-Loaded Micelles
Hiv Reservoirs
topic Anatomical Targeting To the Brain
Cns
Efavirenz-Loaded Micelles
Hiv Reservoirs
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv We investigated the intranasal administration of poly(ethylene oxide)–poly(propylene oxide) polymeric micelles loaded with high payloads of the first-line antiretroviral drug efavirenz for targeting to the CNS. The effect of micellar size and composition and drug payload was assessed, employing simple micelles made of a highly hydrophilic copolymer, poloxamer F127, loaded with 20 mg/ml drug and mixed micelles containing 75% of a medium hydrophobic poloxamine, T904, and 25% F127 loaded with 20 and 30 mg/ml drug, respectively. F127 confers high physical stability, while T904 substantially improves the encapsulation capacity of the micelles. The bioavailability of the drug in the CNS was increased fourfold and the relative exposure index (ratio between the area-under-the-curve in the CNS and plasma) was increased fivefold with respect to the same system administered intravenously. These findings demonstrate the potential of this scalable and cost-viable strategy to attack the HIV sanctuary in the CNS.
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. Oficina de Coordinación Administrativa Houssay; Argentina;
Fil: Hocht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;
Fil: Opezzo, Javier A. W.. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina;
Fil: Sosnik, Alejandro Dario. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina;
description We investigated the intranasal administration of poly(ethylene oxide)–poly(propylene oxide) polymeric micelles loaded with high payloads of the first-line antiretroviral drug efavirenz for targeting to the CNS. The effect of micellar size and composition and drug payload was assessed, employing simple micelles made of a highly hydrophilic copolymer, poloxamer F127, loaded with 20 mg/ml drug and mixed micelles containing 75% of a medium hydrophobic poloxamine, T904, and 25% F127 loaded with 20 and 30 mg/ml drug, respectively. F127 confers high physical stability, while T904 substantially improves the encapsulation capacity of the micelles. The bioavailability of the drug in the CNS was increased fourfold and the relative exposure index (ratio between the area-under-the-curve in the CNS and plasma) was increased fivefold with respect to the same system administered intravenously. These findings demonstrate the potential of this scalable and cost-viable strategy to attack the HIV sanctuary in the CNS.
publishDate 2012
dc.date.none.fl_str_mv 2012-11-22
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/11336/1865
Chiappetta, Diego Andrés; Hocht, Christian; Opezzo, Javier A. W.; Sosnik, Alejandro Dario; Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV; Future Medicine; Nanomedicine; 8; 2; 22-11-2012; 223-237
1743-5889
url http://hdl.handle.net/11336/1865
identifier_str_mv Chiappetta, Diego Andrés; Hocht, Christian; Opezzo, Javier A. W.; Sosnik, Alejandro Dario; Intranasal administration of antiretroviral-loaded micelles for anatomical targeting to the brain in HIV; Future Medicine; Nanomedicine; 8; 2; 22-11-2012; 223-237
1743-5889
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/DOI:10.2217/nnm.12.104
info:eu-repo/semantics/altIdentifier/url/http://www.futuremedicine.com/doi/abs/10.2217/nnm.12.104?url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&rfr_dat=cr_pub%3Dpubmed&
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_ 1846082707630587904
score 13.22299

Publicaciones similares