Transglycosylated rutin-specific non-surface-active nanostructure affects absorption enhancement of flurbiprofen

Transglycosylated rutin (Rutin-G), a newly developed transglycosylated food additive, was used as a novel excipient for improving the dissolution and absorption properties of flurbiprofen. No surface activity was found up to 100 mg/mL of Rutin-G concentration. No cytotoxicity to Caco-2 cells was observed even at a high level of 100 mg/mL Rutin-G solution. 1H NMR study with concentration variation revealed that Rutin-G formed small aggregates in water, with the aggregation number of Rutin-G above the critical aggregation concentration of about 5.0 mg/mL being 4. Structural analyses by small-angle X-ray scattering determined the aggregate to be several nanometers in maximum length. A solubility test of flurbiprofen in the presence of Rutin-G showed that the amount of dissolved flurbiprofen increased in proportion to the amount of Rutin-G loaded. This finding indicated a stoichiometric relationship between flurbiprofen and Rutin-G. The spray-dried particles of flurbiprofen/Rutin-G showed a significantly higher dissolution rate and greater absorption profile compared with the commercial flurbiprofen powder. Taken together, the results indicate the potential application of Rutin-G in the formation of a novel nanostructure of drug/transglycosylated material.

Graphical abstractRutin-G is a potentially useful pharmaceutical excipient due to the characteristic properties such as small aggregate formation without the loss of surface tension and the stoichiometric drug solubilization contributing to enhanced drug absorption.Figure optionsDownload full-size imageDownload high-quality image (241 K)Download as PowerPoint slide