2015 Volume 30 Issue 2 Pages 111-120
The feasibility of trans-glycosylated materials, e.g., α-glucosyl hesperidin, α-glucosyl stevia, and α-glucosyl rutin, to improve the dissolution and bioavailability of poorly water-soluble drug was investigated. Spray-dried particles of drug/trans-glycosylated materials showed a significantly higher dissolution rate and greater absorption profile compared with the commercial drug powder. Molecularly dispersed particles of drug/trans-glycosylated materials may be prepared by spray-drying. We found that trans-glycosylated materials formed different types of aggregated-nanostructures in aqueous media. Trans-glycosylated materials self-associated into particular small micelles with a core-shell like architecture, in which the hydrophobic skeleton is segregated from the aqueous exterior to form a novel drug-loading core surrounded by a hydrophilic shell of sugar groups. The difference in the affinity among drug and associated-nanostructures may relate to the magnitude of solubility enhancement, indicating that the structural similarity of drug and trans-glycosylated materials helped the solubilizing effect.
