Micellization and drug solubilization in aqueous solutions of a diblock copolymer of ethylene oxide and phenyl glycidyl ether.

Pablo Taboada, Gemma Velasquez, Silvia Barbosa, Zhuo Yang, S Keith Nixon, Zhengyuan Zhou, Frank Heatley, Marianne Ashford, Victor Mosquera, David Attwood, Colin Booth

Index: Langmuir 22(18) , 7465-70, (2006)

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Abstract

The aim of this study was to define a block copolymer micellar system with a high solubilization capacity for poorly soluble aromatic drugs. Ethylene oxide and phenyl glycidyl ether were sequentially polymerized to form the diblock copolymer G5E67 (G = phenyl glycidyl ether, OCH2CH(CH2OC6H5); E = oxyethylene, OCH2CH2; subscripts denote number-average block lengths in repeat units). The association properties in aqueous solution over the range 20-50 degrees C were investigated by surface tensiometry and light scattering, yielding values of the cmc, hydrodynamic radius, and association number; gel boundaries in concentrated micellar solution were investigated by tube inversion. The solubilization capacity of G5E67 for the poorly water-soluble drug griseofulvin was higher than that of a triblock EGE copolymer of longer G block length and considerably higher than that achieved with poloxamers (EmPnEm, P = oxypropylene).