Department of Food Science, Purdue University, 745 Agriculture Mall Dr., West Lafayette IN 47906, United States.
Department of Food Science, Purdue University, 745 Agriculture Mall Dr., West Lafayette IN 47906, United States.
Eur J Pharm Sci. 2020 Oct 1;153:105462. doi: 10.1016/j.ejps.2020.105462. Epub 2020 Jul 9.
Curcumin (CCM) is a natural and potent bioactive compound; however, its poor water solubility limits its performances and applications. In this study, octenylsuccinate hydroxypropyl phytoglycogen (OHPP), a dendrimer-like, amphiphilic phytoglycogen derivative, was used to solubilize CCM and enable its inhibitory effect against pathogen Helicobacter pylori. The CCM-OHPP solid dispersion (CCM-OHPP SD) was prepared using spray drying and characterized for its molecular interaction (with FTIR), crystallinity (with X-ray powder diffraction), solubility, and minimal bactericidal concentration (MBC) against three H. pylori strains. The results showed the presence of hydrogen bonds between CCM and OHPP in CCM-OHPP SD and the transformation of CCM from crystalline to amorphous state due to its incorporation with OHPP. For CCM-OHPP SD, the soluble amount of CCM was over 16,000 times that of CCM alone, and the dissolution rate reached 60-99% in 30-60 min. Against three strains of H. pylori, MBC values of CCM were 20 μg/mL for CCM-OHPP SD, which were comparable with that of DMSO-assisted CCM solutions. Overall, the results showed that OHPP was a highly effective solubilizer of CCM to enable its inhibitory efficacy against H. pylori.
姜黄素(CCM)是一种天然的、有效的生物活性化合物;然而,其较差的水溶性限制了它的性能和应用。在本研究中,辛烯基琥珀酸羟丙基支链淀粉(OHPP),一种树状大分子样的两亲性支链淀粉衍生物,被用于溶解 CCM 并使其对病原体幽门螺杆菌的抑制作用成为可能。CCM-OHPP 固体分散体(CCM-OHPP SD)是通过喷雾干燥制备的,并对其分子相互作用(FTIR)、结晶度(X 射线粉末衍射)、溶解度和最小杀菌浓度(MBC)进行了表征,以对抗三种 H. pylori 菌株。结果表明,CCM-OHPP SD 中 CCM 与 OHPP 之间存在氢键,并且由于与 OHPP 的结合,CCM 从结晶态转变为无定形态。对于 CCM-OHPP SD,CCM 的溶解度超过 CCM 单独存在时的 16000 倍,在 30-60 分钟内溶解率达到 60-99%。对于三种 H. pylori 菌株,CCM-OHPP SD 的 CCM 的 MBC 值为 20 μg/mL,与 DMSO 辅助的 CCM 溶液相当。总体而言,结果表明,OHPP 是 CCM 的高效增溶剂,使其对 H. pylori 的抑制作用成为可能。