Song Xuening, Luo Yingting, Zhao Wenduo, Liu Simiao, Wang Yuzhuo, Zhang Hao
College of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, China.
Beijing Laboratory of Food Quality and Safety, Department of Nutrition and Health, China Agricultural University, Beijing 100091, China.
Foods. 2024 Jun 26;13(13):2029. doi: 10.3390/foods13132029.
Lutein is an oxygenated fat-soluble carotenoid and a functional compound with proven health benefits for the human body. Nevertheless, the poor water solubility and low oral bioavailability of lutein greatly limit its application. To address this, we developed an effective approach to enhance the water solubility of lutein through co-amorphous formulation. Specifically, the lutein-sucralose co-amorphous mixture was prepared at a molar ratio of 1:1 using ethanol and water as solvents by employing the solvent evaporation method, followed by solid-state characterization and dissolution testing conducted to assess the properties of the formulation. The X-ray diffraction pattern with an amorphous halo and the differential scanning calorimetry thermogram with no sharp melting peaks confirmed the formation of a binary co-amorphous system. Changes in peak shape, position, and intensity observed in the Fourier transform infrared spectroscopy spectrum revealed intermolecular interactions between lutein and sucralose molecules, while molecular dynamics simulations identified interaction sites between their hydroxyl groups. Additionally, dissolution testing demonstrated better dissolution performance of lutein in the co-amorphous form compared to pure lutein and physical mixture counterparts. Our findings present a novel strategy for improving the water solubility of lutein to make better use of it.
叶黄素是一种含氧的脂溶性类胡萝卜素，是一种对人体健康有益已得到证实的功能性化合物。然而，叶黄素较差的水溶性和较低的口服生物利用度极大地限制了其应用。为了解决这一问题，我们开发了一种通过共无定形制剂来提高叶黄素水溶性的有效方法。具体而言，采用溶剂蒸发法，以乙醇和水为溶剂，按照1:1的摩尔比制备了叶黄素 - 三氯蔗糖共无定形混合物，随后进行固态表征和溶出度测试以评估该制剂的性能。具有非晶晕的X射线衍射图谱和没有尖锐熔融峰的差示扫描量热法热谱图证实了二元共无定形体系的形成。在傅里叶变换红外光谱中观察到的峰形、位置和强度的变化揭示了叶黄素和三氯蔗糖分子之间的分子间相互作用，而分子动力学模拟确定了它们羟基之间的相互作用位点。此外，溶出度测试表明，与纯叶黄素和物理混合物相比，共无定形形式的叶黄素具有更好的溶出性能。我们的研究结果提出了一种提高叶黄素水溶性以更好利用它的新策略。
