Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique

Autores
Seremeta, Katia Pamela; Höcht, Christian; Taira, Carlos Alberto; Cortez Tornello, Pablo Roberto; Abraham, Gustavo Abel; Sosnik, Alejandro Dario
Año de publicación
2015
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
The goal of this study was to investigate the electrohydrodynamic atomization (EHDA) technology to encapsulate the water-soluble antiretroviral didanosine (ddI) within poly(epsilon-caprolactone) (PCL) particles and stabilize it in the gastric medium where it undergoes fast degradation. A preliminary study employing a one-needle setup enabled the adjustment of the critical process parameters. Then, a configuration of two concentric needles named coaxial electrohydrodynamic atomization (CEHDA) led to the formation of ddI-loaded PCL microcapsules. Scanning electron microscopy analysis showed that the microparticles were spherical and with narrow size distribution. Attenuated total reflectance/Fourier transform infrared spectroscopy confirmed that most of the drug was efficiently encapsulated within the particles, whereas differential scanning calorimetry and X-ray powder diffraction revealed that the drug was preserved mainly in crystalline form. The loading capacity was relatively high (approximately 12% w/w), and the encapsulation efficiency was approximately 100%. In vitro release assays (PBS pH ¼ 7.4) indicated that ddI was released almost completely within 2 h. Moreover, the delayed release was expected to isolate ddI from the biological fluids during the gastric transit. Finally, pharmacokinetics studies in rats showed that ddI-loaded particles lead to a statistically significant increase of the oral bioavailability of almost 4 times and a 2-fold prolongation of the half-life with respect to a ddI aqueous solution, supporting the use of CEHDA as a promising reproducible, scalable and cost-viable technology to encapsulate water-soluble drugs within polymeric particles.
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. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Cortez Tornello, Pablo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); Argentina
Fil: Abraham, Gustavo Abel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); Argentina
Fil: Sosnik, Alejandro Dario. Technion-Israel Institute of Technology. Department of Materials Science and Engineering. Group of Pharmaceutical Nanomaterials Science; Israel
Materia
Hiv/Aids
Didanosine
Poly(Epsilon-Caprolactone)
Electrohydrodynamic Atomization
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:11336/6592

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network_name_str CONICET Digital (CONICET)
spelling Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) techniqueSeremeta, Katia PamelaHöcht, ChristianTaira, Carlos AlbertoCortez Tornello, Pablo RobertoAbraham, Gustavo AbelSosnik, Alejandro DarioHiv/AidsDidanosinePoly(Epsilon-Caprolactone)Electrohydrodynamic Atomizationhttps://purl.org/becyt/ford/2.5https://purl.org/becyt/ford/2https://purl.org/becyt/ford/2.9https://purl.org/becyt/ford/2The goal of this study was to investigate the electrohydrodynamic atomization (EHDA) technology to encapsulate the water-soluble antiretroviral didanosine (ddI) within poly(epsilon-caprolactone) (PCL) particles and stabilize it in the gastric medium where it undergoes fast degradation. A preliminary study employing a one-needle setup enabled the adjustment of the critical process parameters. Then, a configuration of two concentric needles named coaxial electrohydrodynamic atomization (CEHDA) led to the formation of ddI-loaded PCL microcapsules. Scanning electron microscopy analysis showed that the microparticles were spherical and with narrow size distribution. Attenuated total reflectance/Fourier transform infrared spectroscopy confirmed that most of the drug was efficiently encapsulated within the particles, whereas differential scanning calorimetry and X-ray powder diffraction revealed that the drug was preserved mainly in crystalline form. The loading capacity was relatively high (approximately 12% w/w), and the encapsulation efficiency was approximately 100%. In vitro release assays (PBS pH ¼ 7.4) indicated that ddI was released almost completely within 2 h. Moreover, the delayed release was expected to isolate ddI from the biological fluids during the gastric transit. Finally, pharmacokinetics studies in rats showed that ddI-loaded particles lead to a statistically significant increase of the oral bioavailability of almost 4 times and a 2-fold prolongation of the half-life with respect to a ddI aqueous solution, supporting the use of CEHDA as a promising reproducible, scalable and cost-viable technology to encapsulate water-soluble drugs within polymeric particles.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. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; ArgentinaFil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; ArgentinaFil: Cortez Tornello, Pablo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); ArgentinaFil: Abraham, Gustavo Abel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); ArgentinaFil: Sosnik, Alejandro Dario. Technion-Israel Institute of Technology. Department of Materials Science and Engineering. Group of Pharmaceutical Nanomaterials Science; IsraelRoyal Society of Chemistry2015-08info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/6592Seremeta, Katia Pamela; Höcht, Christian; Taira, Carlos Alberto; Cortez Tornello, Pablo Roberto; Abraham, Gustavo Abel; et al.; Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique; Royal Society of Chemistry; Journal Of Materials Chemistry B; 3; 1; 8-2015; 102-1112050-7518enginfo:eu-repo/semantics/altIdentifier/url/http://pubs.rsc.org/en/Content/ArticleLanding/2015/TB/c4tb00664jinfo:eu-repo/semantics/altIdentifier/doi/info:eu-repo/semantics/altIdentifier/doi/10.1039/C4TB00664Jinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:52:16Zoai:ri.conicet.gov.ar:11336/6592instacron: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 09:52:16.379CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
title Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
spellingShingle Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
Seremeta, Katia Pamela
Hiv/Aids
Didanosine
Poly(Epsilon-Caprolactone)
Electrohydrodynamic Atomization
title_short Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
title_full Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
title_fullStr Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
title_full_unstemmed Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
title_sort Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique
dc.creator.none.fl_str_mv Seremeta, Katia Pamela
Höcht, Christian
Taira, Carlos Alberto
Cortez Tornello, Pablo Roberto
Abraham, Gustavo Abel
Sosnik, Alejandro Dario
author Seremeta, Katia Pamela
author_facet Seremeta, Katia Pamela
Höcht, Christian
Taira, Carlos Alberto
Cortez Tornello, Pablo Roberto
Abraham, Gustavo Abel
Sosnik, Alejandro Dario
author_role author
author2 Höcht, Christian
Taira, Carlos Alberto
Cortez Tornello, Pablo Roberto
Abraham, Gustavo Abel
Sosnik, Alejandro Dario
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Hiv/Aids
Didanosine
Poly(Epsilon-Caprolactone)
Electrohydrodynamic Atomization
topic Hiv/Aids
Didanosine
Poly(Epsilon-Caprolactone)
Electrohydrodynamic Atomization
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.5
https://purl.org/becyt/ford/2
https://purl.org/becyt/ford/2.9
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv The goal of this study was to investigate the electrohydrodynamic atomization (EHDA) technology to encapsulate the water-soluble antiretroviral didanosine (ddI) within poly(epsilon-caprolactone) (PCL) particles and stabilize it in the gastric medium where it undergoes fast degradation. A preliminary study employing a one-needle setup enabled the adjustment of the critical process parameters. Then, a configuration of two concentric needles named coaxial electrohydrodynamic atomization (CEHDA) led to the formation of ddI-loaded PCL microcapsules. Scanning electron microscopy analysis showed that the microparticles were spherical and with narrow size distribution. Attenuated total reflectance/Fourier transform infrared spectroscopy confirmed that most of the drug was efficiently encapsulated within the particles, whereas differential scanning calorimetry and X-ray powder diffraction revealed that the drug was preserved mainly in crystalline form. The loading capacity was relatively high (approximately 12% w/w), and the encapsulation efficiency was approximately 100%. In vitro release assays (PBS pH ¼ 7.4) indicated that ddI was released almost completely within 2 h. Moreover, the delayed release was expected to isolate ddI from the biological fluids during the gastric transit. Finally, pharmacokinetics studies in rats showed that ddI-loaded particles lead to a statistically significant increase of the oral bioavailability of almost 4 times and a 2-fold prolongation of the half-life with respect to a ddI aqueous solution, supporting the use of CEHDA as a promising reproducible, scalable and cost-viable technology to encapsulate water-soluble drugs within polymeric particles.
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. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Höcht, Christian. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina
Fil: Taira, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
Fil: Cortez Tornello, Pablo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); Argentina
Fil: Abraham, Gustavo Abel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigación En Ciencia y Tecnología de Materiales (i); Argentina
Fil: Sosnik, Alejandro Dario. Technion-Israel Institute of Technology. Department of Materials Science and Engineering. Group of Pharmaceutical Nanomaterials Science; Israel
description The goal of this study was to investigate the electrohydrodynamic atomization (EHDA) technology to encapsulate the water-soluble antiretroviral didanosine (ddI) within poly(epsilon-caprolactone) (PCL) particles and stabilize it in the gastric medium where it undergoes fast degradation. A preliminary study employing a one-needle setup enabled the adjustment of the critical process parameters. Then, a configuration of two concentric needles named coaxial electrohydrodynamic atomization (CEHDA) led to the formation of ddI-loaded PCL microcapsules. Scanning electron microscopy analysis showed that the microparticles were spherical and with narrow size distribution. Attenuated total reflectance/Fourier transform infrared spectroscopy confirmed that most of the drug was efficiently encapsulated within the particles, whereas differential scanning calorimetry and X-ray powder diffraction revealed that the drug was preserved mainly in crystalline form. The loading capacity was relatively high (approximately 12% w/w), and the encapsulation efficiency was approximately 100%. In vitro release assays (PBS pH ¼ 7.4) indicated that ddI was released almost completely within 2 h. Moreover, the delayed release was expected to isolate ddI from the biological fluids during the gastric transit. Finally, pharmacokinetics studies in rats showed that ddI-loaded particles lead to a statistically significant increase of the oral bioavailability of almost 4 times and a 2-fold prolongation of the half-life with respect to a ddI aqueous solution, supporting the use of CEHDA as a promising reproducible, scalable and cost-viable technology to encapsulate water-soluble drugs within polymeric particles.
publishDate 2015
dc.date.none.fl_str_mv 2015-08
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/11336/6592
Seremeta, Katia Pamela; Höcht, Christian; Taira, Carlos Alberto; Cortez Tornello, Pablo Roberto; Abraham, Gustavo Abel; et al.; Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique; Royal Society of Chemistry; Journal Of Materials Chemistry B; 3; 1; 8-2015; 102-111
2050-7518
url http://hdl.handle.net/11336/6592
identifier_str_mv Seremeta, Katia Pamela; Höcht, Christian; Taira, Carlos Alberto; Cortez Tornello, Pablo Roberto; Abraham, Gustavo Abel; et al.; Didanosine-loaded poly(epsilon-caprolactone) microparticles by a coaxial electrohydrodynamic atomization (CEHDA) technique; Royal Society of Chemistry; Journal Of Materials Chemistry B; 3; 1; 8-2015; 102-111
2050-7518
dc.language.none.fl_str_mv eng
language eng
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info:eu-repo/semantics/altIdentifier/doi/
info:eu-repo/semantics/altIdentifier/doi/10.1039/C4TB00664J
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
application/pdf
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dc.publisher.none.fl_str_mv Royal Society of Chemistry
publisher.none.fl_str_mv Royal Society of Chemistry
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
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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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