Pectin-chitosan conjugated nanoliposome as a promising delivery system for neohesperidin: Characterization, release behavior, cellular uptake, and antioxidant property

Neohesperidin (NH) is a flavanone glycoside compound possessing diverse biological activities. However, NH is unstable in physiological condition and poorly soluble in water, and thereby it may show limited bioavailability. The aim of the present study was to facilitate the controlled delivery of NH in simulated gastrointestinal (GI) tract with enhanced cellular uptake using biopolymer conjugation onto nanoliposome (NL). The carrier systems were characterized by dynamic light scattering, HPLC analysis, and Fourier transform infrared spectroscopy. The biological activity was analyzed by in vitro antioxidant activity, rhodamine (Rh123)-assisted cellular uptake, and acrylamide (AA)-induced ROS model on Caco-2 cells. The results confirmed the size of nanocarriers fall in the range of 87-225 nm, well-encapsulation of NH, and conjugation of chitosan (CH) and pectin (P). In vitro digestion study revealed that P and CH-conjugated-nanoliposomes (P-CH-NL) significantly controlled the NH release following by anomalous diffusion mechanism, and preserved around 72-78% of NH in GI condition. The ABTS antioxidant activity, DPPH free radical scavenging capacity, and ferric reducing activity indicated that conjugated-nanoliposomes can preserve greater antioxidant activity after GI digestion. In vitro cellular uptake study showed enhanced Rh123 uptake by carrier systems, particularly P-CH-NL exhibited the highest uptake of around 141% followed by CH-NL (129%) and NL (100%). Cytotoxicity results also exposed that conjugated-nanoliposomes can significantly protect the human Caco-2 cells from AA-induced ROS generation. Conclusively, this work provides a promising approach for the controlled delivery of lipophilic natural products with enhanced cellular uptake at colonic epithelial cells and greater biological activity.