School of Food Science and Engineering, Shaanxi University of Science and Technology, Weiyang University Park, Xi'an 710021, People's Republic of China.
Department of Pharmacy, The First Hospital of China Medical University, Shenyang 110001, People's Republic of China.
Int J Biol Macromol. 2023 Aug 1;245:125489. doi: 10.1016/j.ijbiomac.2023.125489. Epub 2023 Jun 20.
Supersaturating drug delivery system (SDDS) is a promising approach to enhance the solubility of hydrophobic functional components. However, SDDS is thermodynamically unstable and crystallization tends to occur. In this work, curcumin was used as a model compound, and the crystallization inhibitory effect of konjac glucomannan (KGM), sodium alginate (SA) and xanthan gum (XTG) on curcumin in supersaturated solution was investigated. Amorphous solubility of curcumin was determined using ultraviolet extinction, fluorescence spectroscopy and dynamic light scattering methods. Nucleation induction time (NIT) and crystal growth rate of curcumin were evaluated using ultraviolet probe in the absence and presence of various natural polysaccharides (NPs). Results showed that amorphous solubility of curcumin was approximately 30 μg/mL in pH 6.8 phosphate buffer. NPs used in this work restrained nucleation or crystal growth of curcumin effectively. The NITs of curcumin in the absence of NPs and in the presence of XTG, KGM and SA (1 μg/mL) were 3.7, 60.7, 20.0 and 8.0 min, respectively. The crystal growth rate of curcumin in the absence of NPs and in the presence of XTG, SA and KGM (1 μg/mL) were 0.0103, 0.00752, 0.00286 and 0.000306 min, respectively. The nucleation inhibitory effect of NPs on curcumin was ranked as XTG > KGM > SA. The order of crystal growth inhibition capacity of NPs was KGM > SA > XTG. In conclusion, NPs could be incorporated into SDDS to maintain supersaturation of hydrophobic components for enhanced bioavailability.
超饱和药物递送系统 (SDDS) 是提高疏水性功能成分溶解度的一种很有前途的方法。然而，SDDS 在热力学上是不稳定的，容易发生结晶。在这项工作中，姜黄素被用作模型化合物，研究了魔芋葡甘聚糖（KGM）、海藻酸钠（SA）和黄原胶（XTG）对超饱和溶液中姜黄素结晶的抑制作用。使用紫外消光、荧光光谱和动态光散射方法测定姜黄素的无定形溶解度。在有无各种天然多糖（NPs）的情况下，使用紫外探针评估姜黄素的成核诱导时间（NIT）和晶体生长速率。结果表明，在 pH 6.8 磷酸盐缓冲液中，姜黄素的无定形溶解度约为 30μg/mL。本文所用 NPs 有效抑制了姜黄素的成核或晶体生长。在没有 NPs 的情况下和在 XTG、KGM 和 SA（1μg/mL）存在的情况下，姜黄素的 NIT 分别为 3.7、60.7、20.0 和 8.0min。在没有 NPs 的情况下和在 XTG、SA 和 KGM（1μg/mL）存在的情况下，姜黄素的晶体生长速率分别为 0.0103、0.00752、0.00286 和 0.000306min。NPs 对姜黄素的成核抑制作用大小顺序为 XTG>KGM>SA。 NPs 对晶体生长的抑制能力大小顺序为 KGM>SA>XTG。综上所述，NPs 可被纳入 SDDS 以维持疏水性成分的超饱和度，从而提高生物利用度。
