Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment

Miltefosine presents antineoplastic activity but high hemolytic potential. Its use in cancer has been limited to treating cutaneous metastasis of breast cancer. To decrease hemolytic potential, we developed a formulation of miltefosine-loaded polymeric micelles (PM) of the copolymer Pluronic-F127. A...

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Autores: Valenzuela Oses, Johanna K., García, Mónica Cristina, Feitosa, Valker A., Pachioni Vasconcelos, Juliana A., Gomes-Filho, Sandro M., Lourenço, Felipe R., Cerize, Natalia N.P., Bassères, Daniela S., Rangel-Yagui, Carlota O.
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2017
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/65640
Acceso en línea:http://hdl.handle.net/11336/65640
Access Level:acceso abierto
Palabra clave:Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
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spelling Development and characterization of miltefosine-loaded polymeric micelles for cancer treatmentValenzuela Oses, Johanna K.García, Mónica CristinaFeitosa, Valker A.Pachioni Vasconcelos, Juliana A.Gomes-Filho, Sandro M.Lourenço, Felipe R.Cerize, Natalia N.P.Bassères, Daniela S.Rangel-Yagui, Carlota O.AlkylphosphocholinesBlock-CopolymerCancer TherapyHemolytic PotentialMiltefosinePolymeric Micelleshttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2Miltefosine presents antineoplastic activity but high hemolytic potential. Its use in cancer has been limited to treating cutaneous metastasis of breast cancer. To decrease hemolytic potential, we developed a formulation of miltefosine-loaded polymeric micelles (PM) of the copolymer Pluronic-F127. A central composite design was applied and the analysis of variance showed that the optimum level of hydrodynamic diameter and polydispersity index predicted by the model and experimentally confirmed were 29 nm and 0.105, respectively. Thermal analyses confirmed that miltefosine was molecularly dispersed within PM. Pluronic-F127 PM with miltefosine 80 μM presented a significant reduction of hemolytic effect (80%, p < 0.05) in comparison to free drug. In vitro assays against HeLa carcinoma cells demonstrated similar cytotoxicity to free miltefosine and PM. Our results suggest that, by lowering hemolytic potential, miltefosine-loaded Pluronic-F127 PM a promising alternative to broaden this drug use in cancer therapy, as well as of other alkylphosphocholines.Fil: Valenzuela Oses, Johanna K.. Universidade de Sao Paulo; BrasilFil: García, Mónica Cristina. 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: Feitosa, Valker A.. Universidade de Sao Paulo; Brasil. Institute for Technological Research; BrasilFil: Pachioni Vasconcelos, Juliana A.. Universidade de Sao Paulo; BrasilFil: Gomes-Filho, Sandro M.. Universidade de Sao Paulo; BrasilFil: Lourenço, Felipe R.. Universidade de Sao Paulo; BrasilFil: Cerize, Natalia N.P.. Institute for Technological Research; BrasilFil: Bassères, Daniela S.. Universidade de Sao Paulo; BrasilFil: Rangel-Yagui, Carlota O.. Universidade de Sao Paulo; BrasilElsevier Science2017-12info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/65640Valenzuela Oses, Johanna K.; García, Mónica Cristina; Feitosa, Valker A.; Pachioni Vasconcelos, Juliana A.; Gomes-Filho, Sandro M.; et al.; Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment; Elsevier Science; Materials Science and Engineering: C; 81; 12-2017; 327-3330928-4931CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://linkinghub.elsevier.com/retrieve/pii/S0928493117320921info:eu-repo/semantics/altIdentifier/doi/10.1016/j.msec.2017.07.040info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2024-05-08T13:35:18Zoai:ri.conicet.gov.ar:11336/65640instacron: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:34982024-05-08 13:35:19.035CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
title Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
spellingShingle Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
Valenzuela Oses, Johanna K.
Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
title_short Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
title_full Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
title_fullStr Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
title_full_unstemmed Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
title_sort Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment
dc.creator.none.fl_str_mv Valenzuela Oses, Johanna K.
García, Mónica Cristina
Feitosa, Valker A.
Pachioni Vasconcelos, Juliana A.
Gomes-Filho, Sandro M.
Lourenço, Felipe R.
Cerize, Natalia N.P.
Bassères, Daniela S.
Rangel-Yagui, Carlota O.
author Valenzuela Oses, Johanna K.
author_facet Valenzuela Oses, Johanna K.
García, Mónica Cristina
Feitosa, Valker A.
Pachioni Vasconcelos, Juliana A.
Gomes-Filho, Sandro M.
Lourenço, Felipe R.
Cerize, Natalia N.P.
Bassères, Daniela S.
Rangel-Yagui, Carlota O.
author_role author
author2 García, Mónica Cristina
Feitosa, Valker A.
Pachioni Vasconcelos, Juliana A.
Gomes-Filho, Sandro M.
Lourenço, Felipe R.
Cerize, Natalia N.P.
Bassères, Daniela S.
Rangel-Yagui, Carlota O.
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
topic Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
description Miltefosine presents antineoplastic activity but high hemolytic potential. Its use in cancer has been limited to treating cutaneous metastasis of breast cancer. To decrease hemolytic potential, we developed a formulation of miltefosine-loaded polymeric micelles (PM) of the copolymer Pluronic-F127. A central composite design was applied and the analysis of variance showed that the optimum level of hydrodynamic diameter and polydispersity index predicted by the model and experimentally confirmed were 29 nm and 0.105, respectively. Thermal analyses confirmed that miltefosine was molecularly dispersed within PM. Pluronic-F127 PM with miltefosine 80 μM presented a significant reduction of hemolytic effect (80%, p < 0.05) in comparison to free drug. In vitro assays against HeLa carcinoma cells demonstrated similar cytotoxicity to free miltefosine and PM. Our results suggest that, by lowering hemolytic potential, miltefosine-loaded Pluronic-F127 PM a promising alternative to broaden this drug use in cancer therapy, as well as of other alkylphosphocholines.
publishDate 2017
dc.date.none.fl_str_mv 2017-12
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/11336/65640
Valenzuela Oses, Johanna K.; García, Mónica Cristina; Feitosa, Valker A.; Pachioni Vasconcelos, Juliana A.; Gomes-Filho, Sandro M.; et al.; Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment; Elsevier Science; Materials Science and Engineering: C; 81; 12-2017; 327-333
0928-4931
CONICET Digital
CONICET
url http://hdl.handle.net/11336/65640
identifier_str_mv Valenzuela Oses, Johanna K.; García, Mónica Cristina; Feitosa, Valker A.; Pachioni Vasconcelos, Juliana A.; Gomes-Filho, Sandro M.; et al.; Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment; Elsevier Science; Materials Science and Engineering: C; 81; 12-2017; 327-333
0928-4931
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://linkinghub.elsevier.com/retrieve/pii/S0928493117320921
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.msec.2017.07.040
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 Elsevier Science
publisher.none.fl_str_mv Elsevier Science
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
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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