Novel poly(ethylene oxide)-b-poly(propylene oxide) copolymer-glucose conjugate by the microwave-assisted ring opening of a sugar lactone.

GLISONI R.J.; SOSNIK A

MACROMOLECULAR BIOSCIENCE

WILEY-V C H VERLAG GMBH

Lugar: Weinheim; Año: 2014 vol. 14 p. 1639 - 1651

1616-5187

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.