Preparation and Characterization of Lutein Co-Amorphous Formulation with Enhanced Solubility and Dissolution

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.

Keywords

• lutein
• sucralose
• co-amorphous
• solubility enhancement
• rotary evaporation