Preparation and Characterization of Quercetin‐Loaded Zein Nanoparticles by Electrospraying and Study of In Vitro Bioavailability

Abstract

Quercetin is a hydrophobic flavonoid with high antioxidant activity. However, for biological applications, the bioavailability of quercetin is low due to physiological barriers. For this reason, an alternative is the protection of quercetin in matrices of biopolymers as zein. The objective of this work was to prepare and characterize quercetin‐loaded zein nanoparticles by electrospraying and its study of in vitro bioavailability. The physicochemical parameters such as viscosity, density, and electrical conductivity of zein solutions showed a dependence of the ethanol concentration. In addition, rheological parameters demonstrated that solutions of zein in aqueous ethanol present Newtonian behavior, rebounding in the formation of nanoparticles by electrospraying, providing spherical, homogeneous, and compact morphologies, mainly at a concentration of 80% (v/v) of ethanol and of 5% (w/v) of zein. The size and shape of quercetin‐loaded zein nanoparticles were studied by transmission electron microscopy (TEM), observing that it was entrapped, distributed throughout the nanoparticle of zein. Analysis by Fourier transform‐infrared (FT‐IR) of zein nanoparticles loaded with quercetin revealed interactions via hydrogen bonds. The efficacy of zein nanoparticles to entrap quercetin was particularly high for all quercetin concentration evaluated in this work (87.9 ± 1.5% to 93.0 ± 2.6%). The in vitro gastrointestinal release of trapped quercetin after 240 min was 79.1%, while that for free quercetin was 99.2%. The in vitro bioavailability was higher for trapped quercetin (5.9%) compared to free quercetin (1.9%), than of gastrointestinal digestion. It is concluded, that the electrospraying technique made possible the obtention of quercitin‐loaded zein nanoparticles increasing their bioavailability. Practical Application This type of nanosystems can be used in the food and pharmaceutical industry. Quercetin‐loaded zein nanoparticles for its improvement compared to free quercetin can be used to decrease the prevalence of chronic degenerative diseases by increasing of the bioavailability of quercetin in the bloodstream. Other application can be as an antioxidant system in functional foods or oils to increase shelf life.

Effects of different alcohol and ultrasonic treatments on thermal and structural properties of zein‐starch sodium octenyl succinate composite nanoparticles

“…There is a variety of proteins that can be used to fabricate nanoparticles for delivery and emulsification systems, such as caseinate, soy proteins, whey proteins, and zein (Cheng, Mario, & Jones, 2019). Zein, as an inert macromolecule, has been exploited in numerous commercial applications using a wide variety of methods such as electrospinning (Wang et al, 2020), film-casting (Teerakarn et al, 2010), solution blow spinning (Liu et al, 2016), and electrospraying (Francisco et al, 2019;Kang et al, 2021), as well as the anti-solvent precipitation (ASP), liquid-liquid dispersion, electroplating (Joye et al, 2013), and anti-solvent nanoprecipitation technique (Pascoli et al, 2018). Nanoparticles prepared by electrospraying and anti-solvent precipitation have a spherical and compact morphology with the size distribution of 10-447 nm (Francisco et al, 2019;Jiang et al, 2019).…”

Novel extraction, rapid assessment and bioavailability improvement of quercetin: A review

“…The researcher determined in vitro gastrointestinal release of trapped QUR up to 79.1%, while, for free QUR it was 99.2%. The in vitro bioavailability was 5.9% for trapped while 1.9% for the free QUR, displaying better results with QUR zein NPs [103] .…”

“…Other than physical, chemical, and physiological properties including temperature, oxygen, and enzymatic activity of QUR, chemical instability and high biodegradability at different pH of the stomach has encouraged the researchers to preserve it in the hydrophobic matrices as NPs [103] , [104] . Among the natural polymer-based NPs, protein-based NPs are considered easy for the gastrointestinal tract [105] .…”

Natural Products That Target the Arginase in Leishmania Parasites Hold Therapeutic Promise

“…Several approaches have been investigated to enhance quercetin's oral bioavailability to enable its use as a pharmaceutic. The compound's bioavailability has been improved using creative formulations such as quercetin-loaded lipid liquid crystalline systems [89], quercetin-loaded zein nanoparticles and nanoliposomal encapsulation [90]. In vivo studies with Leishmania infected rodents also demonstrated improved efficacy with delivery of quercetin in lipid-core nanocapsules [86] or by combining the oral delivery of the flavonoid with injections of its carrier serum albumin [69].…”