Anhui University of Chinese Medicine, Hefei, 230012, China.
Yangtze Delta Drug Advanced Research Institute, Nantong, 226000, China.
AAPS PharmSciTech. 2024 Jun 11;25(5):135. doi: 10.1208/s12249-024-02853-3.
Lutein (Lut) is a recognized nutritional supplement known for its antioxidative and anti-inflammatory properties, crucial in mitigating ocular disease. However, enhancements to Lut stability and solubility remain challenges to be addressed in the healthcare industry. Herein, we fabricated and evaluated a food-grade highly porous β-cyclodextrin metal-organic framework (β-CD-MOF) for its ability to encapsulate Lut. Lut stability considerably improved when loaded into β-CD-MOF to form a Lut@β-CD-MOF complex, which exhibited better stability than Lut loaded into the γ-cyclodextrin metal-organic framework (Lut@γ-CD-MOF), Lut@β-CD, and commercial product (Blackmores™) at 40°C, 60°C, and 70°C, respectively. The solubility of Lut@β-CD-MOF in water increased by 26.8-fold compared to raw Lut at 37°C. Lut@β-CD-MOF exhibited greater hydrophilicity, as determined by measuring the water contact angle. Molecular docking and other characterizations of Fourier transform infrared spectroscopy and powder X-ray diffraction confirmed that Lut was successfully encapsulated in the chamber formed by the three cyclodextrins in β-CD-MOF. Thermogravimetric analysis and Raman spectroscopy demonstrated that Lut distributed in the β-CD-MOF cavity deeply improved Lut stability and solubility. In conclusion, our findings underscored the function of β-CD-MOF in enhancing Lut stability and solubility for formulation applications.
叶黄素 (Lut) 是一种公认的营养补充剂,具有抗氧化和抗炎特性,对于减轻眼部疾病至关重要。然而,提高 Lut 的稳定性和溶解度仍然是医疗保健行业需要解决的挑战。在此,我们制备并评估了一种食品级的高多孔β-环糊精金属有机骨架 (β-CD-MOF),以评估其包封 Lut 的能力。当 Lut 负载到 β-CD-MOF 中形成 Lut@β-CD-MOF 复合物时,其稳定性得到了显著提高,与负载到γ-环糊精金属有机骨架 (Lut@γ-CD-MOF)、β-CD 负载的 Lut 和商业产品 (Blackmores™) 相比,在 40°C、60°C 和 70°C 下的稳定性更好。在 37°C 时,Lut@β-CD-MOF 在水中的溶解度比原始 Lut 提高了 26.8 倍。通过测量水接触角,Lut@β-CD-MOF 表现出更大的亲水性。分子对接和傅里叶变换红外光谱及粉末 X 射线衍射等其他特性表明,Lut 成功地被包封在β-CD-MOF 中由三个环糊精形成的腔室中。热重分析和拉曼光谱表明,Lut 分布在β-CD-MOF 腔中,极大地提高了 Lut 的稳定性和溶解度。总之,我们的研究结果强调了β-CD-MOF 在增强 Lut 稳定性和溶解度方面的作用,为制剂应用提供了参考。
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