Lutein Loaded in β-Cyclodextrin Metal-Organic Frameworks for Stability and Solubility Enhancements
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.
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Material
Lut (purity: ≥80%) was obtained from Nanjing Jingzhu Biotechnology Co., Ltd. (Jiangsu, China). Lut tablets (Blackmores™, Lot number: 313,047) were procured from Blackmores Co., Ltd. (Sydney, Australia). β-CD was sourced from Qufu Tianli Medical Supplement Co., Ltd. (Shandong, China). γ-CD was supplied by Maxdragon Biochem Co., Ltd. (Guangdong, China). Analytical grade potassium hydroxide (KOH), potassium acetate (KAc), glacial acetic acid, methanol (MeOH), ethanol (EtOH), and ethyl acetate were obtained from Sinopharm Chemical Reagent Co., Ltd. (Shanghai, China). Chromatographic-grade MeOH was purchased from Meryer Chemical Technologies Co., Ltd. (Shanghai, China). Purified water was generated using a reverse osmosis unit of a Milli-Q water purification system (Master-S15UV, Hetai Instrument Co., Ltd., Shanghai, China).
Zhang, H., Dong, L., Guo, T. et al. Lutein Loaded in β-Cyclodextrin Metal-Organic Frameworks for Stability and Solubility Enhancements. AAPS PharmSciTech 25, 135 (2024). https://doi.org/10.1208/s12249-024-02853-3
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