Nanocomposite formation between alpha-glucosyl stevia and surfactant improves the dissolution profile of poorly water-soluble drug

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• 作者：Hiromasa Uchiyama ; Yuichi Tozuka ; Masahiro Nishikawa ; Hirofumi Takeuchi ; ^{takeuchi@gifu-pu.ac.jp}
• 关键词：伪-glucosyl stevia ; Flurbiprofen ; Surfactant ; Dissolution enhancement ; Nanocomposite
• 刊名：International Journal of Pharmaceutics
• 出版年：2012
• 期刊代码：24_03785173
• 类别：pha
• 出版时间：30 May, 2012
• 卷：428
• 期：1-2
• 页码：183-186
• 文件大小：478 K

摘要

The formation of a hybrid-nanocomposite using 伪-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-尾-d-maltopyranoside. To investigate the dissolution-enhancement effect of Stevia-G/SDS mixture, the pyrene I₁/I₃ ratio was plotted versus the Stevia-G concentration. The pyrene I₁/I₃ 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.