title: Nanocomposite formation between alpha-glucosyl stevia and surfactant improves the dissolution profile of poorly water-soluble drug.
abstract: The formation of a hybrid-nanocomposite using α-glucosyl stevia (Stevia-G) and surfactant was explored to improve the dissolution of flurbiprofen (FP). As reported previously, the dissolution amount of FP was enhanced in the presence of Stevia-G, induced by the formation of an FP and Stevia-G-associated nanostructure. When a small amount of sodium dodecyl sulfate (SDS) was present with Stevia-G, the amount of dissolved FP was extremely enhanced. This dissolution-enhancement effect was also observed with the cationic surfactant of dodecyl trimethyl ammonium bromide, but not with the non-ionic surfactant of n-octyl-β-D-maltopyranoside. To investigate the dissolution-enhancement effect of Stevia-G/SDS mixture, the pyrene I(1)/I(3) ratio was plotted versus the Stevia-G concentration. The pyrene I(1)/I(3) ratio of Stevia-G/SDS mixture had a sigmoidal curve at lower Stevia-G concentrations compared to the Stevia-G solution alone. These results indicate that the Stevia-G/SDS mixture provides a hydrophobic core around pyrene molecules at lower Stevia-G concentrations, leading to nanocomposite formation between Stevia-G and SDS. The nanocomposite of Stevia-G/SDS showed no cytotoxicity to Caco-2 cells at a mixture of 0.1% SDS and 1% Stevia-G solution, whereas 0.1% SDS solution showed high toxicity. These results suggest that the nanocomposite formation of Stevia-G/SDS may be useful way to enhance the dissolution of poorly water-soluble drugs without special treatment.
authors.affiliation: Gifu Pharmaceutical University, 1-25-4 Daigaku-nishi, Gifu 501-1196, Japan.
authors.forename: Hiromasa
authors.initials: H
authors.lastname: Uchiyama
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Tozuka
authors.forename: Masahiro
authors.initials: M
authors.lastname: Nishikawa
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Takeuchi
mesh_terms: D018938:Caco-2 Cells; D005480:Flurbiprofen / Q000737:chemistry*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008320:Maltose / Q000031:analogs & derivatives / Q000737:chemistry; D008823:Micelles; D053761:Nanocomposites / Q000737:chemistry*; D011721:Pyrenes / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D036625:Stevia / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*; D013816:Thermodynamics; D014867:Water / Q000737:chemistry*
chemical_list: D008823:Micelles; D011721:Pyrenes; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; D014867:Water; D012967:Sodium Dodecyl Sulfate; D005480:Flurbiprofen; D008320:Maltose; C104928:octyl maltopyranoside; C030984:pyrene; C022806:dodecyltrimethylammonium