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Título: | Polymeric drugs based on random copolymers with antimitotic activity |
Autor: | López-Donaire, M. L. CSIC ORCID; Parra-Cáceres, J.; Fernández-Gutiérrez, Mar CSIC ORCID ; Vázquez Lasa, Blanca; San Román, Julio CSIC | Fecha de publicación: | 2010 | Editor: | American Chemical Society | Citación: | Biomacromolecules 11 : 2478–2486 (2010) | Resumen: | Polymeric drugs based on random copolymers with antimitotic activity were obtained by free radical copolymerization of oleyl 2-acetamido-2-deoxy-R-D-glucopyranoside methacrylate (OAGMA) and 2-ethyl-(2- pyrrolidone) methacrylate (EPM) at low and high conversion and analyzed in terms of microstructure, physicochemical, and biological properties. Reactivity ratios of monomers were found to be rOAGMA ) 1.34 and rEPM ) 0.98, indicating the obtaining of statistical copolymers with random sequence distribution of the comonomeric units in the macromolecular chains. The glass transition temperature of the copolymers presents a negative deviation from the predicted values according to the Fox equation, suggesting a higher flexibility of the alternating diad. Copolymeric systems with OAGMA contents between 10-50 mol % presented thermosensitive behavior in a heating process showing cloud point temperatures (CPT) in the range 45-28 °C with increasing OAGMA content and hysteresis in one heating-and-cooling cycle. In vitro glycolipid release studies revealed the stability of the ester group in culture medium. The polymeric drugs with 30 and 50 mol % OAGMA presented antimitotic activity on a human glioblastoma line, but they were less toxic on normal human fibroblast cultures. | Versión del editor: | http://dx.doi.org/10.1021/bm100672c | URI: | http://hdl.handle.net/10261/56453 | DOI: | 10.1021/bm100672c | ISSN: | 1525-7797 | E-ISSN: | 1526-4602 |
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