Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols

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Molecules 2020, 25, 4613 19 of 36 Pharmacokinetic analysis in mice showed that the oral availability of curcumin from the nanoemulsion was nine times higher than that of unformulated curcumin, and the digestion of the nanoemulsion in the gastrointestinal tract was significantly faster than that of the organogel. Another team used ultrasound to prepare a curcumin-nanoemulsion. In a gastrointestinal simulation experiment, the release rate of curcumin from the nanoemulsion was slower, because the nanoemulsion was not easily hydrolyzed by pepsin, and pancreatin can cause its release [274]. Similarly, Zou et al. [275] studied the potential of three nano-drug delivery systems, nanoemulsion, zein nanosuspension and nanoliposomes, to improve curcumin bioavailability. The study found that curcumin loaded into nanoemulsion was most effective for gastrointestinal absorption. In one study, EGCG encapsulated in an oil/water nanoemulsion exhibited significantly increased anticancer activity in vitro compared with free EGCG, and the droplet size of the nanoemulsion hardly changed over 14 days [276]. In another study, the authors investigated the effects of nanoemulsion encapsulation on the physical and chemical properties, biological activity, and epithelial permeability of EGCG. Compared with unencapsulated catechins, the bioaccessibility of EGCG-nanoemulsion increased by 2.78 times. In addition, the intestinal permeability of EGCG was significantly increased. These results showed that a soybean protein nanoemulsion could improve the stability, bioaccessibility and permeability of green tea catechin [277]. Although nanoemulsions have significant advantages, they are unstable at low pH, and their small size and liquid nature make drug release difficult to control. In addition, the preparation of nanoemulsions requires specialized equipment, so there is a perception in the food industry that nanoemulsions are unprofitable [14]. 3.8. Metal Nanoparticles Compared with organic nanoparticles, inorganic nanoparticles have unique characteristics, such as good controllability of size and shape, large specific surface area, and imaging potential. They also enable targeted drug delivery and synergistic therapy. These characteristics make them well suited for drug delivery. Among all inorganic nanoparticles, metal nanoparticles are the most widely used. Metal nanoparticles are composed of pure metals such as gold, silver or platinum, with a size of 1–100 nm. In recent years, they have attracted increasing attention due to their huge potential in drug delivery systems [278,279]. 3.8.1. Gold Nanoparticles (AuNPs) Gold nanoparticles are crystal structures composed of metal gold atoms, and are the most widely used metal nanoparticles, with many properties that make them the most promising nanomaterials in biomedical fields such as biosensors, molecular imaging and drug carriers. They are 1–100 nm in size, and form a variety of shapes such as ball, bar and cage. In addition, they are non-toxic, biocompatible, are negatively charged and easily functionalized by other biomolecules [280–282]. Traditional gold nanoparticles are synthesized using chemicals that are harmful to human health and the environment [283]. In recent years, numerous gold nanoparticles have been prepared using plant active compounds that are friendly to the human body and the environment, such as polyphenols [284]. Curcumin (Cur) is the most widely used plant active compound in the preparation of gold nanoparticles (Figure 10).

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