Novel Poly(Ethylene Oxide)-b-Poly(Propylene Oxide) Copolymer-Glucose Conjugate by the Microwave-Assisted Ring Opening of a Sugar Lactone

In this work, we investigated for the first time the conjugation of gluconolactone to a poly(ethylene oxide)-poly(propylene oxide) block copolymer by a microwave-assisted ring opening reaction. The glucosylated copolymer was obtained with high yield(90%). A conjugation extent of approximately 100% w...

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Detalles Bibliográficos
Autores: Glisoni, Romina Julieta, Sosnik, Alejandro Dario
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2014
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/30659
Acceso en línea:http://hdl.handle.net/11336/30659
Access Level:acceso abierto
Palabra clave:Gluconolactone
Polymeric Micelles
Darunavir
Mw Assisted Synthesis
https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
Descripción
Sumario:In this work, we investigated for the first time the conjugation of gluconolactone to a poly(ethylene oxide)-poly(propylene oxide) block copolymer by a microwave-assisted ring opening reaction. The glucosylated copolymer was obtained with high yield(90%). A conjugation extent of approximately 100% was achieved within 15 min. The modification reduced the critical micellar concentration and increased the size of the micelles. The agglutination of the modified polymeric micelles by a soluble lectin that binds glucose confirmed the recognizability of the modified nanocarrier. Finally, the solubilization of darunavir, an anti-HIV protease inhibitor, showed a sharp increase of the aqueous solubility from 91 microgram/mL to 14.2 and 18.9 mg/mL for 10% w/v pristine and glucosylated polymeric micelles, respectively.