Study on the bioavailability of stevioside-encapsulized lutein and its mechanism

• Published in: Food chemistry Vol. 354; p. 129528
• Main Authors: Dai, Zhuqing, Song, Jiangfeng, Chen, Ye, Feng, Lei, Xu, Yayuan, Li, Dajing, Wu, Caie, Zhang, Zhongyuan, Liu, Jun
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 30-08-2021
• Subjects: Animals; Bioavailability; Biological Availability; Caco-2 Cells; Capsules - chemistry; Diterpenes, Kaurane - chemistry; Glucosides - chemistry; Humans; Lutein; Lutein - chemistry; Mechanism; Mice; Molecular Docking Simulation; Nanoparticle; Stevioside; Structural characteristics; Lutein; Stevioside; Bioavailability; Structural characteristics; Nanoparticle; Mechanism
• ISSN: 0308-8146; 1873-7072
• DOI: 10.1016/j.foodchem.2021.129528

•The Lutein:OH-Stevioside:O hydrogen bond, CHπ interaction and van der Waals forces make lutein(LUT) well placed in the hydrophobic cavity of stevioside(STE) and form the LUT-STE nanoparticles.•In vitro Caco-2 cell model and in vivo mice pharmacokinetics model showed the stevioside nano-entrapment significantly promote the bioavailability of lutein.•The LUT-STE enter into cells mainly through passive diffusion, as well as clathrin-mediated endocytosis and caveolae/lipid raft dependent endocytosis.•CD36, NPC1L1 and PPARγ play important roles in the transmembrane pathway of LUT-STE.
This study aims to develop novel lutein nanoparticles encapsulized by stevioside (LUT-STE, 165 ± 2 nm average particles size) and systematically evaluate its bioavailability. Multiple spectroscopy and NMR analyses showed lutein and stevioside could interact through hydrogen bonds, CHπ interaction and van der Waals forces. Molecular docking simulation showed lutein was well distributed in the hydrophobic cavity of stevioside. Analyzed by Caco-2 cellular models, the transported amount of LUT-STE was 2.39 times that of lutein in 120 min with a Papp (B → A)/Papp (A → B) value of 0.63 ± 0.04. Nystatin and dynasore significantly reduced the cellular uptake of LUT-STE by 41.3% and 57.7%, respectively. Compared with free lutein, LUT-STE increased the Cmax in mice plasma by 5.01-fold and promoted the accumulation in multiple organs. LUT-STE promoted the protein expressions of CD36, NPC1L1 and PPARγ in both cell and animal models. In conclusion, stevioside entrapment significantly promote the bioavailability of lutein through multiple transmembrane pathways.