Stabilization of a non-aqueous self-double-emulsifying delivery system of rutin by fat crystals and nonionic surfactants: preparation and bioavailability study

Abstract

Literature examples of non-aqueous Pickering emulsions stabilized by fat crystals are very rare. Moreover, the applications of rutin are limited due to its low solubility in both water and oils (less than 0.10 mg g and 0.25 mg g, respectively). Thus, herein, we developed an optimum formulation of a non-aqueous self-double-emulsifying delivery system (SDEDS) containing rutin and evaluated its oral bioavailability. The new formulation stabilized by fat crystals (glycerol monostearate, GMS) and nonionic surfactants was prepared via a two-step emulsification process. The presence of a mixture of GMS crystals and nonionic surfactants effectively improves the stability of the emulsions. The non-aqueous SDEDS spontaneously forms oil-in-oil-in-water (O/O/W) double emulsions in the gastrointestinal environment with the inner oil phase mainly containing the active ingredients. It is stable at both 4 °C and 25 °C for 30 days and could enhance the dissolution properties of the active ingredients. Furthermore, the protection of rutin against digestion-mediated precipitation was observed when the formulation contained a high concentration of GMS crystals. The oral absolute bioavailability of rutin obtained from SDEDS (8.62%) is 1.76-fold higher than that of the actives suspension (4.90%). Thus, the non-aqueous SDEDS is an attractive candidate for the encapsulation of water-insoluble and simultaneously oil-insoluble nutrients (such as rutin) and for use in oral delivery applications.

Improved stability of (W1/O/W2) double emulsions based on dual gelation: Oleogels and hydrogels

“…This study proposed a new method to improve the stability of double emulsions by the combination of oleogels and hydrogels. Compared to previous studies, this method could obtain stable double emulsions reinforced by oleogels with a low content of hydrophilic emulsifier and an applicable dispersibility (Wang et al, ; Zhao et al, ). Nonetheless, when employing this method, the composition of oleogels and hydrogels and technological parameter should be carefully investigated, because of the complex effects of solid lipids and alginate on double emulsions.…”

“…In addition, lipid crystals could also improve the stability of primary emulsions through the Pickering effect as Pickering lipid crystals (Frasch‐Melnik, Spyropoulos, & Norton, ). It has been reported that GMS, which was an interfacially active emulsifier with a high melting point, was able to hinder the collision and the coalescence of droplets by creating crystal shells around the dispersed droplets (Ghosh & Rousseau, ; Wang et al, ). In general, the relative importance of these two roles was dependent on the presence of an appropriate emulsifier to facilitate the interfacial nucleation of solid lipids (Nadin et al, ).…”

“…ing point, was able to hinder the collision and the coalescence of droplets by creating crystal shells around the dispersed droplets (Ghosh & Rousseau, 2012;Wang et al, 2017). In general, the relative importance of these two roles was dependent on the presence of an appropriate emulsifier to facilitate the interfacial nucleation of solid lipids (Nadin et al, 2014).…”

“…It has been reported that triglycerides, monoglycerides, and fatty alcohols could be employed as the lipid‐based gelator to produce the lipid crystal network in lipid phase, which could solidify the oil globules, reinforce the oil film, and hinder the coalescence of inner droplets, thereby improving the stability of double emulsions (Andrade, Wright, & Corredig, ; Herzi & Essafi, ; Nadin, Rousseau, & Ghosh, ). In our previous studies, we have developed double emulsions containing crystal monoglyceride network using a self‐emulsifying method to enhance the stability of double emulsions through two paths: the reinforcement of the thin oil film and the avoidance of oil globule coalescence (Wang et al, ; Zhao et al, ). Although these systems improved the stability of double emulsions, the potential application of them was limited by the high content of hydrophilic emulsifier and the inferior dispersibility.…”

Solid Self‐Emulsifying Delivery System (S‐SEDS) of Dihydromyricetin: A New Way for Preparing Functional Food

“…The antioxidant activity of DMY and DMY‐loaded S‐SEDS was evaluated based on the ability to scavenge DPPH free radical according to the modified method reported by Wang, Huang, et al. (). Briefly, 100 µL of aqueous suspensions of DMY‐loaded S‐SEDS or DMY ethanol solution was mixed with 3.9 ml of DPPH ethanol solution (30 µg/ml).…”