PDF(Pubmed)
Abstract：
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.
摘要：
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的功能性化合物。然而，叶黄素水溶性差、口服生物利用度低,极大地限制了其应用。为了解决这个问题，我们开发了一种有效的方法来提高叶黄素的水溶性通过共无定形制剂。具体来说,以乙醇和水为溶剂，采用溶剂蒸发法，以1:1的摩尔比制备叶黄素-三氯半乳蔗糖共无定形混合物，然后进行固态表征和溶出测试以评估制剂的性质。具有无定形晕轮的X射线衍射图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。峰形变化,position,在傅里叶变换红外光谱中观察到的强度揭示了叶黄素和三氯半乳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的羟基之间的相互作用位点。此外,溶出测试表明，与纯叶黄素和物理混合物对应物相比，共无定形形式的叶黄素具有更好的溶出性能。我们的发现提出了一种改善叶黄素水溶性以更好地利用它的新策略。
