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 100mg/mL of Rutin-G concentration. No cytotoxicity to Caco-2 cells was observed even at a high level of 100mg/mL Rutin-G solution. (1)H 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 5.0mg/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.
Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, Gifu, Japan.
Yuichi
Y
Tozuka
Kenjirou
K
Higashi
Takeshi
T
Morita
Masahiro
M
Nishikawa
Hiromasa
H
Uchiyama
Junying
J
Zhang
Kunikazu
K
Moribe
Keiko
K
Nishikawa
Hirofumi
H
Takeuchi
Keiji
K
Yamamoto
D000818:Animals; D018938:Caco-2 Cells; D004305:Dose-Response Relationship, Drug; D005079:Excipients / Q000737:chemistry*; D005480:Flurbiprofen / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000633:toxicity; D006031:Glycosylation; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D049329:Nanostructures; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012431:Rutin / Q000737:chemistry*; D012995:Solubility
D005079:Excipients; D012431:Rutin; D005480:Flurbiprofen