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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Detalles Bibliográficos
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
Descripción
Sumario: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.