Flavonoids exhibited diverse biological activity via modulating several signaling pathways. But there are various therapeutic limitations such as physiological instability, low bioavailability, etc. that restricted the use of flavonoids. Liposomes are non-toxic, biodegradable, self-assembled lipid vesicular system that has long and versatile applications in foods, cosmetics, and pharmaceuticals industry. Nevertheless, traditional liposomes are easily oxidized during storage conditions and thereby release the cargo. Traditional liposomes are also unstable at low pH and enzymatic conditions. Surface decoration of conventional liposomes by different biopolymers can improve stability by reducing environmental degradation and phospholipid bilayer permeation during storage conditions and in the biological systems. In the present study, nanoliposomal system was formed using a thin-layered hydration method with probe sonication approach, whereas pectin (P) and chitosan (CH) coating were added by layer-by-layer electrostatic approach. In this study, neohesperidin (NH, lipophilic compound) and pelargonidin-3-O-glucoside (Pg, hydrophilic compound) were used as model flavonoids. Different nanoliposomal systems, i.e. nanoliposome (NL), CH-coated NL (CH-NL), and P-coated CH-NL (P-CH-NL) were characterized through DLS, HPLC, TEM, DSC, and FTIR. Thereafter, we evaluated the physicochemical stability of liposomal systems under storage, thermal, pH, ionic, UV, oxidative, and serum conditions. We further evaluated the delivery of liposomal systems using Caco2 and L02 cells, respectively. Our characterization results confirmed the good encapsulation efficiency (&gt; 90%) and successful layer formation with the nano-sized and spherical carrier. Both CH-NL and P-CH-NL exhibited better physicochemical stability than NL under storage, thermal, pH, ionic, UV, oxidative, and serum conditions. In vitro gastrointestinal digestion study revealed that P-CH-NL provided better protection to compounds compared to NL and CH-NL, respectively. In contrast, NH-loaded P-CH-NL exhibited good in vitro mucoadhesive property, higher cellular uptake to Caco2 cells, and exerted better ROS reduction capacity in AA-induced Caco2 cells. Collectively, our results unveil that pectin-chitosan-coated nanoliposomal system can be a suitable alternative delivery system for flavonoids for the controlled delivery and greater biological activity.

Pectin-chitosan-coated nanoliposome is a promising nanocarrier for encapsulation, controlled delivery, and enhanced biological activity of food bioactive compounds

ACS Fall 2021

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