Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery

Autores
Udabe, Jakes; Martin-Saldaña, Sergio; Tao, Yushi; Picchio, Matías Luis; Beloqui, Ana; Paredes, Alejandro Javier; Calderón, Marcelo
Año de publicación
2024
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Nanocrystals (NCs) have entirely changed the panorama ofhydrophobic drug delivery, showing improved biopharmaceutical performancethrough multiple administration routes. NCs are potential highly loaded nanovectorsdue to their pure drug composition, standing out from conventional polymers andlipid nanoparticles that have limited drug-loading capacity. However, research in thisarea is limited. This study introduces the concept of surface modification of drugNCs through single-layer poly(ethylene glycol) (PEG) polymerization as aninnovative strategy to boost targeting efficiency. The postpolymerization analysisrevealed size and composition alterations, indicating successful surface engineeringof NCs of the model drug curcumin of approximately 200 nm. Interestingly, mucosaltissue penetration analysis showed enhanced entry for fully coated and low crosslinked(LCS) PEG NCs, with an increase of 15 μg/cm2 compared to the controlNCs. In addition, we found that polymer chemistry variations on the NCs’ surfacenotably impacted mucin binding, with those armored with LCS PEG showing the most significant reduction in interaction with thisglycoprotein. We validated this strategy in an in vitro nose-to-brain model, with all of the NCs exhibiting a promising ability to crossa tight monolayer. Furthermore, the metabolic and pro-inflammatory activity revealed clear indications that, despite surfacemodifications, the efficacy of curcumin remains unaffected. These findings highlight the potential of surface PEGylated NCs intargeted drug delivery. Altogether, this work sets the baseline for further exploration and optimization of surface polymerized NCsfor enhanced drug delivery applications, promising more efficient treatments for specific disorders and conditions requiring activetargeting.
Fil: Udabe, Jakes. Universidad del Pais Vasco. Polymat.; España
Fil: Martin-Saldaña, Sergio. Universidad del Pais Vasco. Polymat.; España
Fil: Tao, Yushi. The Queens University of Belfast; Irlanda
Fil: Picchio, Matías Luis. Universidad Tecnológica Nacional. Facultad Regional Villa María. Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina
Fil: Beloqui, Ana. Universidad del Pais Vasco. Polymat.; España
Fil: Paredes, Alejandro Javier. The Queens University of Belfast; Irlanda. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Calderón, Marcelo. Universidad del Pais Vasco. Polymat.; España
Materia
Nanocrystals
Surface chemistry
Nose-to-brain route
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/264100
Acceder
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repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted DeliveryUdabe, JakesMartin-Saldaña, SergioTao, YushiPicchio, Matías LuisBeloqui, AnaParedes, Alejandro JavierCalderón, MarceloNanocrystalsSurface chemistryNose-to-brain routehttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2Nanocrystals (NCs) have entirely changed the panorama ofhydrophobic drug delivery, showing improved biopharmaceutical performancethrough multiple administration routes. NCs are potential highly loaded nanovectorsdue to their pure drug composition, standing out from conventional polymers andlipid nanoparticles that have limited drug-loading capacity. However, research in thisarea is limited. This study introduces the concept of surface modification of drugNCs through single-layer poly(ethylene glycol) (PEG) polymerization as aninnovative strategy to boost targeting efficiency. The postpolymerization analysisrevealed size and composition alterations, indicating successful surface engineeringof NCs of the model drug curcumin of approximately 200 nm. Interestingly, mucosaltissue penetration analysis showed enhanced entry for fully coated and low crosslinked(LCS) PEG NCs, with an increase of 15 μg/cm2 compared to the controlNCs. In addition, we found that polymer chemistry variations on the NCs’ surfacenotably impacted mucin binding, with those armored with LCS PEG showing the most significant reduction in interaction with thisglycoprotein. We validated this strategy in an in vitro nose-to-brain model, with all of the NCs exhibiting a promising ability to crossa tight monolayer. Furthermore, the metabolic and pro-inflammatory activity revealed clear indications that, despite surfacemodifications, the efficacy of curcumin remains unaffected. These findings highlight the potential of surface PEGylated NCs intargeted drug delivery. Altogether, this work sets the baseline for further exploration and optimization of surface polymerized NCsfor enhanced drug delivery applications, promising more efficient treatments for specific disorders and conditions requiring activetargeting.Fil: Udabe, Jakes. Universidad del Pais Vasco. Polymat.; EspañaFil: Martin-Saldaña, Sergio. Universidad del Pais Vasco. Polymat.; EspañaFil: Tao, Yushi. The Queens University of Belfast; IrlandaFil: Picchio, Matías Luis. Universidad Tecnológica Nacional. Facultad Regional Villa María. Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; ArgentinaFil: Beloqui, Ana. Universidad del Pais Vasco. Polymat.; EspañaFil: Paredes, Alejandro Javier. The Queens University of Belfast; Irlanda. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Calderón, Marcelo. Universidad del Pais Vasco. Polymat.; EspañaAmerican Chemical Society2024-08info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/264100Udabe, Jakes; Martin-Saldaña, Sergio; Tao, Yushi; Picchio, Matías Luis; Beloqui, Ana; et al.; Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery; American Chemical Society; ACS Applied Materials & Interfaces; 16; 36; 8-2024; 47124-471361944-8244CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/acsami.4c07669info:eu-repo/semantics/altIdentifier/doi/10.1021/acsami.4c07669info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-10T13:01:17Zoai:ri.conicet.gov.ar:11336/264100instacron: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:34982025-09-10 13:01:17.213CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
title Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
spellingShingle Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
Udabe, Jakes
Nanocrystals
Surface chemistry
Nose-to-brain route
title_short Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
title_full Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
title_fullStr Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
title_full_unstemmed Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
title_sort Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery
dc.creator.none.fl_str_mv Udabe, Jakes
Martin-Saldaña, Sergio
Tao, Yushi
Picchio, Matías Luis
Beloqui, Ana
Paredes, Alejandro Javier
Calderón, Marcelo
author Udabe, Jakes
author_facet Udabe, Jakes
Martin-Saldaña, Sergio
Tao, Yushi
Picchio, Matías Luis
Beloqui, Ana
Paredes, Alejandro Javier
Calderón, Marcelo
author_role author
author2 Martin-Saldaña, Sergio
Tao, Yushi
Picchio, Matías Luis
Beloqui, Ana
Paredes, Alejandro Javier
Calderón, Marcelo
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv Nanocrystals
Surface chemistry
Nose-to-brain route
topic Nanocrystals
Surface chemistry
Nose-to-brain route
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv Nanocrystals (NCs) have entirely changed the panorama ofhydrophobic drug delivery, showing improved biopharmaceutical performancethrough multiple administration routes. NCs are potential highly loaded nanovectorsdue to their pure drug composition, standing out from conventional polymers andlipid nanoparticles that have limited drug-loading capacity. However, research in thisarea is limited. This study introduces the concept of surface modification of drugNCs through single-layer poly(ethylene glycol) (PEG) polymerization as aninnovative strategy to boost targeting efficiency. The postpolymerization analysisrevealed size and composition alterations, indicating successful surface engineeringof NCs of the model drug curcumin of approximately 200 nm. Interestingly, mucosaltissue penetration analysis showed enhanced entry for fully coated and low crosslinked(LCS) PEG NCs, with an increase of 15 μg/cm2 compared to the controlNCs. In addition, we found that polymer chemistry variations on the NCs’ surfacenotably impacted mucin binding, with those armored with LCS PEG showing the most significant reduction in interaction with thisglycoprotein. We validated this strategy in an in vitro nose-to-brain model, with all of the NCs exhibiting a promising ability to crossa tight monolayer. Furthermore, the metabolic and pro-inflammatory activity revealed clear indications that, despite surfacemodifications, the efficacy of curcumin remains unaffected. These findings highlight the potential of surface PEGylated NCs intargeted drug delivery. Altogether, this work sets the baseline for further exploration and optimization of surface polymerized NCsfor enhanced drug delivery applications, promising more efficient treatments for specific disorders and conditions requiring activetargeting.
Fil: Udabe, Jakes. Universidad del Pais Vasco. Polymat.; España
Fil: Martin-Saldaña, Sergio. Universidad del Pais Vasco. Polymat.; España
Fil: Tao, Yushi. The Queens University of Belfast; Irlanda
Fil: Picchio, Matías Luis. Universidad Tecnológica Nacional. Facultad Regional Villa María. Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Santa Fe. Instituto de Desarrollo Tecnológico para la Industria Química. Universidad Nacional del Litoral. Instituto de Desarrollo Tecnológico para la Industria Química; Argentina
Fil: Beloqui, Ana. Universidad del Pais Vasco. Polymat.; España
Fil: Paredes, Alejandro Javier. The Queens University of Belfast; Irlanda. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Calderón, Marcelo. Universidad del Pais Vasco. Polymat.; España
description Nanocrystals (NCs) have entirely changed the panorama ofhydrophobic drug delivery, showing improved biopharmaceutical performancethrough multiple administration routes. NCs are potential highly loaded nanovectorsdue to their pure drug composition, standing out from conventional polymers andlipid nanoparticles that have limited drug-loading capacity. However, research in thisarea is limited. This study introduces the concept of surface modification of drugNCs through single-layer poly(ethylene glycol) (PEG) polymerization as aninnovative strategy to boost targeting efficiency. The postpolymerization analysisrevealed size and composition alterations, indicating successful surface engineeringof NCs of the model drug curcumin of approximately 200 nm. Interestingly, mucosaltissue penetration analysis showed enhanced entry for fully coated and low crosslinked(LCS) PEG NCs, with an increase of 15 μg/cm2 compared to the controlNCs. In addition, we found that polymer chemistry variations on the NCs’ surfacenotably impacted mucin binding, with those armored with LCS PEG showing the most significant reduction in interaction with thisglycoprotein. We validated this strategy in an in vitro nose-to-brain model, with all of the NCs exhibiting a promising ability to crossa tight monolayer. Furthermore, the metabolic and pro-inflammatory activity revealed clear indications that, despite surfacemodifications, the efficacy of curcumin remains unaffected. These findings highlight the potential of surface PEGylated NCs intargeted drug delivery. Altogether, this work sets the baseline for further exploration and optimization of surface polymerized NCsfor enhanced drug delivery applications, promising more efficient treatments for specific disorders and conditions requiring activetargeting.
publishDate 2024
dc.date.none.fl_str_mv 2024-08
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/11336/264100
Udabe, Jakes; Martin-Saldaña, Sergio; Tao, Yushi; Picchio, Matías Luis; Beloqui, Ana; et al.; Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery; American Chemical Society; ACS Applied Materials & Interfaces; 16; 36; 8-2024; 47124-47136
1944-8244
CONICET Digital
CONICET
url http://hdl.handle.net/11336/264100
identifier_str_mv Udabe, Jakes; Martin-Saldaña, Sergio; Tao, Yushi; Picchio, Matías Luis; Beloqui, Ana; et al.; Unveiling the Potential of Surface Polymerized Drug Nanocrystals in Targeted Delivery; American Chemical Society; ACS Applied Materials & Interfaces; 16; 36; 8-2024; 47124-47136
1944-8244
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/acsami.4c07669
info:eu-repo/semantics/altIdentifier/doi/10.1021/acsami.4c07669
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv American Chemical Society
publisher.none.fl_str_mv American Chemical Society
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
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score 12.48226

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