A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs

A biodegradable copolyester, poly(butylene succinate-co-e-caprolactone) (PBS_CL), was used for first time as an excipient for pharmaceutical dosage forms using direct compression and hot processing techniques (ultrasound-assisted compression (USAC) and hot melt extrusion (HME)). Robust binary system...

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Autores: Galdón Navarro, Eduardo, Millán Jiménez, Mónica, Mora Castaño, Gloria, Martínez de Ilarduya Sáez de Asteasu, Domingo Antxon|||0000-0001-8105-2168, Caraballo Rodríguez, Isidoro
Tipo de recurso: artículo
Fecha de publicación:2021
País:España
Institución:Universitat Politècnica de Catalunya (UPC)
Repositorio:UPCommons. Portal del coneixement obert de la UPC
Idioma:inglés
OAI Identifier:oai:upcommons.upc.edu:2117/358265
Acceso en línea:https://hdl.handle.net/2117/358265
https://dx.doi.org/10.3390/pharmaceutics13071057
Access Level:acceso abierto
Palabra clave:drugs -- Controlled release
Biomedical materials
Copolymers
Poly(butylene succinate-co-e-caprolactone)
Biodegradable polymer
Ultrasound-assisted compression
Hot melt extrusion
Controlled release
Nanostructured matrices
Medicaments -- Alliberament retardat
Materials biomèdics
Copolímers
Àrees temàtiques de la UPC::Enginyeria química
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spelling A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugsGaldón Navarro, EduardoMillán Jiménez, MónicaMora Castaño, GloriaMartínez de Ilarduya Sáez de Asteasu, Domingo Antxon|||0000-0001-8105-2168Caraballo Rodríguez, Isidorodrugs -- Controlled releaseBiomedical materialsCopolymersPoly(butylene succinate-co-e-caprolactone)Biodegradable polymerUltrasound-assisted compressionHot melt extrusionControlled releaseNanostructured matricesMedicaments -- Alliberament retardatMaterials biomèdicsCopolímersÀrees temàtiques de la UPC::Enginyeria químicaA biodegradable copolyester, poly(butylene succinate-co-e-caprolactone) (PBS_CL), was used for first time as an excipient for pharmaceutical dosage forms using direct compression and hot processing techniques (ultrasound-assisted compression (USAC) and hot melt extrusion (HME)). Robust binary systems were achieved with hot processing techniques, allowing a controlled release of the drug. With only 12% v/v of PBS_CL, controlled release forms were obtained using USAC whereas in HME over 34% v/v of excipient is necessary. Amounts over 23% v/v allowed a long-extended release for more than 72 h following diffusional kinetic. Thanks to the high melting point of theophylline and the physicochemical properties of PBS_CL selected and synthesized, the structure of the excipient inside the USAC tablets and HME filaments corresponds to a continuum medium. A percolation threshold around 23% v/v was estimated, which agrees with a continuum percolation model. The polymer shows a high excipient efficiency value using HME and USAC. A nanostructured matrix with wall thicknesses lower than 0.1 µm was obtained. This leads to a very effective coating of the drug particles by the excipient, providing a slow and reproducible release. The present study therefore supports the use of PBS_CL, for the preparation of controlled release dosage forms using hot processing techniques.Peer ReviewedObjectius de Desenvolupament Sostenible::3 - Salut i Benestar20212021-07-0120212021-12-13journal articlehttp://purl.org/coar/resource_type/c_6501VoRhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/2117/358265https://dx.doi.org/10.3390/pharmaceutics13071057reponame:UPCommons. Portal del coneixement obert de la UPCinstname:Universitat Politècnica de Catalunya (UPC)InglésengAgencia Estatal de Investigación http://doi.org/10.13039/501100011033 Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020 RTI2018-095041-B-C33 SISTEMAS DE LIBERACION DE FARMACOS BASADOS EN POLIMEROS AVANZADOS PARA EL TRATAMIENTO DE ENFERMEDADES GASTROINTESTINALES: POLIESTERES ANFIFILICOS Y BIOPOLIMEROS CARBOXILADOSopen accesshttp://purl.org/coar/access_right/c_abf2Attribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:upcommons.upc.edu:2117/3582652026-05-27T15:37:01Z
dc.title.none.fl_str_mv A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
title A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
spellingShingle A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
Galdón Navarro, Eduardo
drugs -- Controlled release
Biomedical materials
Copolymers
Poly(butylene succinate-co-e-caprolactone)
Biodegradable polymer
Ultrasound-assisted compression
Hot melt extrusion
Controlled release
Nanostructured matrices
Medicaments -- Alliberament retardat
Materials biomèdics
Copolímers
Àrees temàtiques de la UPC::Enginyeria química
title_short A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
title_full A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
title_fullStr A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
title_full_unstemmed A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
title_sort A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
dc.creator.none.fl_str_mv Galdón Navarro, Eduardo
Millán Jiménez, Mónica
Mora Castaño, Gloria
Martínez de Ilarduya Sáez de Asteasu, Domingo Antxon|||0000-0001-8105-2168
Caraballo Rodríguez, Isidoro
author Galdón Navarro, Eduardo
author_facet Galdón Navarro, Eduardo
Millán Jiménez, Mónica
Mora Castaño, Gloria
Martínez de Ilarduya Sáez de Asteasu, Domingo Antxon|||0000-0001-8105-2168
Caraballo Rodríguez, Isidoro
author_role author
author2 Millán Jiménez, Mónica
Mora Castaño, Gloria
Martínez de Ilarduya Sáez de Asteasu, Domingo Antxon|||0000-0001-8105-2168
Caraballo Rodríguez, Isidoro
author2_role author
author
author
author
dc.subject.none.fl_str_mv drugs -- Controlled release
Biomedical materials
Copolymers
Poly(butylene succinate-co-e-caprolactone)
Biodegradable polymer
Ultrasound-assisted compression
Hot melt extrusion
Controlled release
Nanostructured matrices
Medicaments -- Alliberament retardat
Materials biomèdics
Copolímers
Àrees temàtiques de la UPC::Enginyeria química
topic drugs -- Controlled release
Biomedical materials
Copolymers
Poly(butylene succinate-co-e-caprolactone)
Biodegradable polymer
Ultrasound-assisted compression
Hot melt extrusion
Controlled release
Nanostructured matrices
Medicaments -- Alliberament retardat
Materials biomèdics
Copolímers
Àrees temàtiques de la UPC::Enginyeria química
description A biodegradable copolyester, poly(butylene succinate-co-e-caprolactone) (PBS_CL), was used for first time as an excipient for pharmaceutical dosage forms using direct compression and hot processing techniques (ultrasound-assisted compression (USAC) and hot melt extrusion (HME)). Robust binary systems were achieved with hot processing techniques, allowing a controlled release of the drug. With only 12% v/v of PBS_CL, controlled release forms were obtained using USAC whereas in HME over 34% v/v of excipient is necessary. Amounts over 23% v/v allowed a long-extended release for more than 72 h following diffusional kinetic. Thanks to the high melting point of theophylline and the physicochemical properties of PBS_CL selected and synthesized, the structure of the excipient inside the USAC tablets and HME filaments corresponds to a continuum medium. A percolation threshold around 23% v/v was estimated, which agrees with a continuum percolation model. The polymer shows a high excipient efficiency value using HME and USAC. A nanostructured matrix with wall thicknesses lower than 0.1 µm was obtained. This leads to a very effective coating of the drug particles by the excipient, providing a slow and reproducible release. The present study therefore supports the use of PBS_CL, for the preparation of controlled release dosage forms using hot processing techniques.
publishDate 2021
dc.date.none.fl_str_mv 2021
2021-07-01
2021
2021-12-13
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
VoR
http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/2117/358265
https://dx.doi.org/10.3390/pharmaceutics13071057
url https://hdl.handle.net/2117/358265
https://dx.doi.org/10.3390/pharmaceutics13071057
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.relation.none.fl_str_mv Agencia Estatal de Investigación http://doi.org/10.13039/501100011033 Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020 RTI2018-095041-B-C33 SISTEMAS DE LIBERACION DE FARMACOS BASADOS EN POLIMEROS AVANZADOS PARA EL TRATAMIENTO DE ENFERMEDADES GASTROINTESTINALES: POLIESTERES ANFIFILICOS Y BIOPOLIMEROS CARBOXILADOS
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:UPCommons. Portal del coneixement obert de la UPC
instname:Universitat Politècnica de Catalunya (UPC)
instname_str Universitat Politècnica de Catalunya (UPC)
reponame_str UPCommons. Portal del coneixement obert de la UPC
collection UPCommons. Portal del coneixement obert de la UPC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300724

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