Poly (D, L-lactide-co-glycolide)-phospholipid nanocarrier for efficient delivery of macular pigment lutein: absorption pharmacokinetics in mice and antiproliferative effect in Hep G2 cells.

Lutein has various biological activities, its application in food and pharma industries are limited due to poor aqueous solubility, stability, and bioavailability. To achieve various benefits, lutein-poly (lactic-co-glycolic acid) (PLGA)-phospholipid (PL) nanocapsules were prepared. Lutein-PLGA NCs (+PL) were synthesized, characterized and its bioavailability was studied in vitro and in vivo. The cellular uptake and anti-proliferative activity were analyzed in Hep G2 cells. The mean size and zeta value of lutein-PLGA NCs (+PL) were 140 ± 6 nm and - 44 mV. The amorphous nature of lutein in PLGA NCs (+PL) was confirmed by XRD and DSC. In vitro lutein release kinetics showed an initial burst followed by sustainable release up to 86%. In vitro bioavailability showed 62.7% higher lutein bioaccessibility than lutein in free form. The AUC of lutein after single oral dose of lutein-PLGA NCs (+PL) revealed 3.91-fold (plasma), 2.89-fold (liver), and 3.12-fold (eyes) higher absorption than the control (mixed micelles). The IC50 of lutein-PLGA NCs (+PL) in Hep G2 cells at 72 h was 4.5 μM as opposed to 23.4 μM for lutein in free form. Thus, results reveal that PL added to PLGA NCs helps in enhancing the solubility which in turn resulted in its better bioavailability and bioefficacy.