Abstract

Lutein is a hydrophobic antioxidant carotenoid with proven retinal and macular protection against oxidative stress. However, low aqueous solubility and bioavailability limit its clinical application. Hence, focus of the study was to improve the solubility and bioavailability of lutein by using a chitosan-oleic acid-sodium alginate-based nano-carrier system (LNCs). LNCs were prepared by ionic gelation and optimized by Plackett-Burman factorial algorithm. The size and zeta potential of LNCs were characterized by electron microscopy and dynamic light scattering. LNCs were within a size range of 40–160 nm with a desired zeta potential of +45 ± 5 mV and PDI of 0.174 ± 0.02. Further, LNCs displayed 1000-fold higher aqueous solubility with controlled and sustained release kinetics in vitro. Compared to micellar lutein, higher intracellular transport (40%) of lutein from LNCs in Caco-2 cells. Oral gavage of single dose of LNCs in rats resulted in higher (128.3%) bioavailability of lutein compared to micellar lutein. Further, a dose-dependent increase in plasma (135.20, 165.30 nmol/mL) and eyes (1.51 & 3.98 μg/g) was observed upon oral gavage of LNCs (10 and 100 mg/kg BW). Results demonstrate higher solubility and bioavailability of lutein from LNCs and hence could be an efficient therapeutic tool to conquer macular degeneration and retinopathy.

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