Fabrication of chitosan nanoparticles with phosphatidylcholine for improved sustain release, basolateral secretion, and transport of lutein in Caco-2 cells

Abstract

Biopolymers-based nanoparticles delivery emerged alternatively to improve nutraceuticals and drug bioavailability. The intestinal physiology suggested a prerequisite of lipid moiety for carotenoid absorption. This study aimed to fabricate chitosan-based nanoparticles with phosphatidylcholine (PC) to enhance lutein bioavailability. Lutein encapsulated chitosan nanoparticles with PC (LCNPC) or without PC (LCN) were assessed for bioaccessibility, sustain release, cellular uptake/internalization, and basolateral secretion of lutein in Caco-2 cells. Standard lutein mixed micelles (LMM), and micelles derived through in vitro digestion of green leafy vegetables (GMM) treated as controls. The LCNPC showed reduced particle size, higher colloidal stability, homogeneous dispersion, and suitable for oral administration compared to LCN. The cellular uptake of lutein (20 h) in LCNPC was higher than LCN, LMM, and GMM, respectively. Interestingly, lutein uptake was maximum at 8 h in LMM and gradually decreased against sustain-release response in LCNPC and LCN, whereas considerably low lutein uptake from GMM at all time points. Further, LCNPC significantly increased basolateral secretion of triglyceride (TG) and positively correlated enhanced lutein uptake/internalization process than LCN and micelles. Also, LCNPC demonstrated the upregulation of endocytosis, paracellular, scavenger receptor class B type 1 (SRB-1), and peroxisome proliferator-activated receptor gamma (PPARγ) mediated lutein transport mechanism. These results suggested that fabrication of biopolymer-based nanoparticles with PC could provide greater insight to improve lutein bioavailability at enterocyte levels, to avoid age-related macular degeneration and other chronic diseases.