7,8-Dihydroxyflavone nano-liposomes decorated by crosslinked and glycosylated lactoferrin: storage stability, antioxidant activity, in vitro release, gastrointestinal digestion and transport in Caco-2 cell monolayers

Abstract

• 7,8-DHF-Lip-CL-LF and 7,8-DHF-Lip-GC-LF were firstly fabricated. • 7,8-DHF-Lip-GC-LF has high stability and bioaccessibility of 7,8-DHF. • 7,8-DHF-Lip-GC-LF is a promising delivery system for 7,8-DHF. Low bioavailability and stability of 7,8-dihydroxyflavone (7,8-DHF) hinder its potential application in prevention of humans’ disease. 7,8-DHF loaded nanoliposomes decorated by original, crosslinked and glycosylated lactoferrin (LF) were fabricated. The mean particle size of spherical crosslinked and glycosylated LF coating liposomes were larger than uncoated liposomes with a low polydispersity index, and the former had higher encapsulation efficiency (Above 98%). Crosslinked and glycosylated LF coating liposomes had higher antioxidant activity, storage stability, slow-release ability, bioaccessibility and transepithelial transport compared to free 7,8-DHF and 7,8-DHF loaded liposome. Effective hydrogen bonding between phospholipid and 7,8-DHF, while electrostatic interaction and hydrogen bonding between LF proteins and phospholipid existed. The encapsulated 7,8-DHF was in an amorphous state rather than a crystalline form as detected by differential scanning calorimetry. Collectively, crosslinked or glycosylated LF coating liposomes are promising delivery systems for protecting and transporting 7,8-DHF or other relative bioactive components.