Novel Hybrid Inulin-Soy Protein Nanoparticles Simultaneously Loaded with (-)-Epicatechin and Quercetin and Their In Vitro Evaluation.

(-)-Epicatechin and quercetin have attracted considerable attention for their potential therapeutic application in non-communicable chronic diseases. A novel hybrid inulin-soy protein nanoparticle formulation was simultaneously loaded with (-)-epicatechin and quercetin (NEQs) to improve the bioavailability of these flavonoids in the human body, and NEQs were synthesized by spray drying. After process optimization, the physicochemical and functional properties of NEQs were characterized including in vitro release, in vitro gastrointestinal digestion, and cell viability assays. Results showed that NEQs are an average size of 280.17 ± 13.42 nm and have a zeta potential of -18.267 ± 0.83 mV in the organic phase. Encapsulation efficiency of (-)-epicatechin and quercetin reached 97.04 ± 0.01 and 92.05 ± 1.95%, respectively. A 3.5% soy protein content conferred controlled release characteristics to the delivery system. Furthermore, NEQs presented inhibitory effects in Caco-2, but not in HepG-2 and HDFa cell lines. These results contribute to the design and fabrication of inulin-soy protein nanoparticles for improving the bioavailability of multiple bioactive compounds with beneficial properties.

Optimization of the Synthesis of Natural Polymeric Nanoparticles of Inulin Loaded with Quercetin: Characterization and Cytotoxicity Effect.

Quercetin is a bioactive component that is capable of having therapeutic potential in the prevention of different noncommunicable chronic diseases (NCDs). However, it presents instability in the gastrointestinal tract in addition to low bioavailability. One way to overcome the limitations of quercetin lies in using nanotechnology for the development of nanoparticles, based on biopolymers, that are capable of being ingestible. Inulin, a fructan-type polysaccharide, acts as a delivery system for the release of quercetin in a target cell, guaranteeing the stability of the molecule. Inulin-coated quercetin nanoparticles were synthesized by the spray dryer method, and four variables were evaluated, namely inulin concentration (5-10% w/v), feed temperature (40-60 °C), inlet temperature (100-200 °C) and outlet temperature (60-100 °C). The optimal conditions were obtained at 10% w/v inulin concentration, with 45 °C feed temperature, 120 °C inlet temperature and 60 °C outlet temperature, and the nanoparticle size was 289.75 ± 16.3 nm in water. Fluorescence microscopy indicated quercetin loading in the inulin nanoparticles, with an encapsulation efficiency of approximately 73.33 ± 7.86%. Inulin-coated quercetin nanoparticles presented effects of inhibition in Caco-2 and HepG2 cells, but not in HDFa cells. The experimental data showed the potential of inulin nanoparticles as transport materials for unstable molecules, in oral administration systems, for the encapsulation, protection and release of quercetin.

Nanotechnology as a Key to Enhance the Benefits and Improve the Bioavailability of Flavonoids in the Food Industry.

Nanotechnology has impacted the food industry, mainly on developing healthier, safer, and high-quality functional food. Flavonoids are valuable compounds present in plants, fruits, grains, roots, stems, tea, and wine, among others; they possess many benefits for health due to their antioxidant properties toward reactive oxygen species, anti-inflammatory, and antiproliferative, among others. These characteristics make flavonoids attractive in various industrial areas such as medicine, nutraceutical, cosmetology, and pharmaceutical. Unfortunately, flavonoids lack long-term stability, are sensitive to light, long periods of darkness with low oxygen concentration, and often present a low water solubility and poor bioavailability. Nanoencapsulation is an alternative to improve bioavailability and sensitivity in the manufacturing process, based on encapsulating substances on a nanoscale. Nanocapsules are a promising strategy in significantly enhancing the delivery of compounds to various sites in the body. The development of biopolymers to encapsulate sensitive compounds is increasing, as well as the search for the non-toxic, biodegradable, natural and biocompatible characteristics of polymers, is fundamental. The present review describes the recent techniques and technologies for the nanoencapsulation of flavonoids. It discusses their potential advantages and possible limitations, compares natural and synthetic biopolymers, and finally, details nanoparticle regulation.