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

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.
Año de publicación
2017
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
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.
Fil: Valenzuela Oses, Johanna K.. Universidade de Sao Paulo; Brasil
Fil: 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; Argentina
Fil: Feitosa, Valker A.. Universidade de Sao Paulo; Brasil. Institute for Technological Research; Brasil
Fil: Pachioni Vasconcelos, Juliana A.. Universidade de Sao Paulo; Brasil
Fil: Gomes-Filho, Sandro M.. Universidade de Sao Paulo; Brasil
Fil: Lourenço, Felipe R.. Universidade de Sao Paulo; Brasil
Fil: Cerize, Natalia N.P.. Institute for Technological Research; Brasil
Fil: Bassères, Daniela S.. Universidade de Sao Paulo; Brasil
Fil: Rangel-Yagui, Carlota O.. Universidade de Sao Paulo; Brasil
Materia
Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
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:11336/65640
Acceder
id CONICETDig_7e190df435fdfda69e31ad5f2329ca85
oai_identifier_str oai:ri.conicet.gov.ar:11336/65640
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
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 Técnicas2025-10-15T14:24:58Zoai: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:34982025-10-15 14:24:59.085CONICET 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
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
topic Alkylphosphocholines
Block-Copolymer
Cancer Therapy
Hemolytic Potential
Miltefosine
Polymeric Micelles
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv 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.
Fil: Valenzuela Oses, Johanna K.. Universidade de Sao Paulo; Brasil
Fil: 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; Argentina
Fil: Feitosa, Valker A.. Universidade de Sao Paulo; Brasil. Institute for Technological Research; Brasil
Fil: Pachioni Vasconcelos, Juliana A.. Universidade de Sao Paulo; Brasil
Fil: Gomes-Filho, Sandro M.. Universidade de Sao Paulo; Brasil
Fil: Lourenço, Felipe R.. Universidade de Sao Paulo; Brasil
Fil: Cerize, Natalia N.P.. Institute for Technological Research; Brasil
Fil: Bassères, Daniela S.. Universidade de Sao Paulo; Brasil
Fil: Rangel-Yagui, Carlota O.. Universidade de Sao Paulo; Brasil
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
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
_version_ 1846082678376366080
score 13.22299

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