Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide

Autores
Quinteros, Daniela Alejandra; Ferreira, Luana M.; Schaffazick, Scheila Rezende; Palma, Santiago Daniel; Allemandi, Daniel Alberto; Cruz, Letícia
Año de publicación
2016
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Glaucoma is characterized by increased intraocular pressure (IOP) that results in blindness if it remains untreated. Acetazolamide (AZM) is a carbonic anhydrase inhibitor, mainly used to reduce IOP in the treatment of glaucoma. However, the potential of topical treatment is limited, due to its low permeability across the ocular epithelium. An alternative to overcome this limitation is the incorporation of AZM in nanoparticulate systems, such as polymeric nanocapsules (NCs). In this way, the aim of this work was to prepare and characterize NC formulations containing AZM, using ethylcellulose (EC) and Eudragit® RS100 (EUD) as encapsulating polymers. The formulations showed high encapsulation efficiency. Particle size measurements showed that NCs are in the nanometric range. Comparing both groups of formulations, the NCEC proved to be smaller than those prepared with EUD. The formulations prepared with EC showed negative zeta potentials, while NCs of EUD were positively charged. For both groups of formulations, no more than 30% of drug was released in 120 min. Ex vivo and in vivo studies evidenced that the NCEC formulations were the most efficient, because an increased amount of permeated drug was observed, along with a greater IOP decrease and longer duration of the effect in normotensive rabbits.
Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Ferreira, Luana M.. Universidade Federal de Santa Maria; Brasil
Fil: Schaffazick, Scheila Rezende. Universidade Federal de Santa Maria; Brasil
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Cruz, Letícia. Universidade Federal de Santa Maria; Brasil
Materia
Drug Delivery Systems
Nanocapsules
Nanotechnology
Ophthalmic Drug Delivery
Polymeric Drug Delivery Systems
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/62986
Acceder
id CONICETDig_59908d66f76b17273e2d548602b49e28
oai_identifier_str oai:ri.conicet.gov.ar:11336/62986
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of AcetazolamideQuinteros, Daniela AlejandraFerreira, Luana M.Schaffazick, Scheila RezendePalma, Santiago DanielAllemandi, Daniel AlbertoCruz, LetíciaDrug Delivery SystemsNanocapsulesNanotechnologyOphthalmic Drug DeliveryPolymeric Drug Delivery Systemshttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2Glaucoma is characterized by increased intraocular pressure (IOP) that results in blindness if it remains untreated. Acetazolamide (AZM) is a carbonic anhydrase inhibitor, mainly used to reduce IOP in the treatment of glaucoma. However, the potential of topical treatment is limited, due to its low permeability across the ocular epithelium. An alternative to overcome this limitation is the incorporation of AZM in nanoparticulate systems, such as polymeric nanocapsules (NCs). In this way, the aim of this work was to prepare and characterize NC formulations containing AZM, using ethylcellulose (EC) and Eudragit® RS100 (EUD) as encapsulating polymers. The formulations showed high encapsulation efficiency. Particle size measurements showed that NCs are in the nanometric range. Comparing both groups of formulations, the NCEC proved to be smaller than those prepared with EUD. The formulations prepared with EC showed negative zeta potentials, while NCs of EUD were positively charged. For both groups of formulations, no more than 30% of drug was released in 120 min. Ex vivo and in vivo studies evidenced that the NCEC formulations were the most efficient, because an increased amount of permeated drug was observed, along with a greater IOP decrease and longer duration of the effect in normotensive rabbits.Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Ferreira, Luana M.. Universidade Federal de Santa Maria; BrasilFil: Schaffazick, Scheila Rezende. Universidade Federal de Santa Maria; BrasilFil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Cruz, Letícia. Universidade Federal de Santa Maria; BrasilElsevier2016-10info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/62986Quinteros, Daniela Alejandra; Ferreira, Luana M.; Schaffazick, Scheila Rezende; Palma, Santiago Daniel; Allemandi, Daniel Alberto; et al.; Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide; Elsevier; Journal of Pharmaceutical Sciences; 105; 10; 10-2016; 3183-31900378-5173CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.xphs.2016.06.023info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0022354916415212info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:47:27Zoai:ri.conicet.gov.ar:11336/62986instacron: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 09:47:27.389CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
title Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
spellingShingle Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
Quinteros, Daniela Alejandra
Drug Delivery Systems
Nanocapsules
Nanotechnology
Ophthalmic Drug Delivery
Polymeric Drug Delivery Systems
title_short Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
title_full Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
title_fullStr Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
title_full_unstemmed Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
title_sort Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide
dc.creator.none.fl_str_mv Quinteros, Daniela Alejandra
Ferreira, Luana M.
Schaffazick, Scheila Rezende
Palma, Santiago Daniel
Allemandi, Daniel Alberto
Cruz, Letícia
author Quinteros, Daniela Alejandra
author_facet Quinteros, Daniela Alejandra
Ferreira, Luana M.
Schaffazick, Scheila Rezende
Palma, Santiago Daniel
Allemandi, Daniel Alberto
Cruz, Letícia
author_role author
author2 Ferreira, Luana M.
Schaffazick, Scheila Rezende
Palma, Santiago Daniel
Allemandi, Daniel Alberto
Cruz, Letícia
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Drug Delivery Systems
Nanocapsules
Nanotechnology
Ophthalmic Drug Delivery
Polymeric Drug Delivery Systems
topic Drug Delivery Systems
Nanocapsules
Nanotechnology
Ophthalmic Drug Delivery
Polymeric Drug Delivery Systems
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv Glaucoma is characterized by increased intraocular pressure (IOP) that results in blindness if it remains untreated. Acetazolamide (AZM) is a carbonic anhydrase inhibitor, mainly used to reduce IOP in the treatment of glaucoma. However, the potential of topical treatment is limited, due to its low permeability across the ocular epithelium. An alternative to overcome this limitation is the incorporation of AZM in nanoparticulate systems, such as polymeric nanocapsules (NCs). In this way, the aim of this work was to prepare and characterize NC formulations containing AZM, using ethylcellulose (EC) and Eudragit® RS100 (EUD) as encapsulating polymers. The formulations showed high encapsulation efficiency. Particle size measurements showed that NCs are in the nanometric range. Comparing both groups of formulations, the NCEC proved to be smaller than those prepared with EUD. The formulations prepared with EC showed negative zeta potentials, while NCs of EUD were positively charged. For both groups of formulations, no more than 30% of drug was released in 120 min. Ex vivo and in vivo studies evidenced that the NCEC formulations were the most efficient, because an increased amount of permeated drug was observed, along with a greater IOP decrease and longer duration of the effect in normotensive rabbits.
Fil: Quinteros, Daniela Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Ferreira, Luana M.. Universidade Federal de Santa Maria; Brasil
Fil: Schaffazick, Scheila Rezende. Universidade Federal de Santa Maria; Brasil
Fil: Palma, Santiago Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Allemandi, Daniel Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Cruz, Letícia. Universidade Federal de Santa Maria; Brasil
description Glaucoma is characterized by increased intraocular pressure (IOP) that results in blindness if it remains untreated. Acetazolamide (AZM) is a carbonic anhydrase inhibitor, mainly used to reduce IOP in the treatment of glaucoma. However, the potential of topical treatment is limited, due to its low permeability across the ocular epithelium. An alternative to overcome this limitation is the incorporation of AZM in nanoparticulate systems, such as polymeric nanocapsules (NCs). In this way, the aim of this work was to prepare and characterize NC formulations containing AZM, using ethylcellulose (EC) and Eudragit® RS100 (EUD) as encapsulating polymers. The formulations showed high encapsulation efficiency. Particle size measurements showed that NCs are in the nanometric range. Comparing both groups of formulations, the NCEC proved to be smaller than those prepared with EUD. The formulations prepared with EC showed negative zeta potentials, while NCs of EUD were positively charged. For both groups of formulations, no more than 30% of drug was released in 120 min. Ex vivo and in vivo studies evidenced that the NCEC formulations were the most efficient, because an increased amount of permeated drug was observed, along with a greater IOP decrease and longer duration of the effect in normotensive rabbits.
publishDate 2016
dc.date.none.fl_str_mv 2016-10
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/11336/62986
Quinteros, Daniela Alejandra; Ferreira, Luana M.; Schaffazick, Scheila Rezende; Palma, Santiago Daniel; Allemandi, Daniel Alberto; et al.; Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide; Elsevier; Journal of Pharmaceutical Sciences; 105; 10; 10-2016; 3183-3190
0378-5173
CONICET Digital
CONICET
url http://hdl.handle.net/11336/62986
identifier_str_mv Quinteros, Daniela Alejandra; Ferreira, Luana M.; Schaffazick, Scheila Rezende; Palma, Santiago Daniel; Allemandi, Daniel Alberto; et al.; Novel Polymeric Nanoparticles Intended for Ophthalmic Administration of Acetazolamide; Elsevier; Journal of Pharmaceutical Sciences; 105; 10; 10-2016; 3183-3190
0378-5173
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.xphs.2016.06.023
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0022354916415212
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
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 13.13397

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