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Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols

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Nanoformulations to Enhance the Bioavailability and Physiological Functions of Polyphenols ( nanoformulations-enhance-bioavailability-and-physiological-f )

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Molecules 2020, 25, 4613 12 of 36 Molecules 2020, 23, x FOR PEER REVIEW 12 of 36 Figure 5. (A) Thechemiiccallssttrruucctuturreeooffththeegeglealtaitni.n(.B(B) )ScSacnaninigngelelcetrcotrnonmmicriocrsocoscpoyp(ySE(SME)Mim) iamgeasgeosf pouf rpeucrheictohsiatonssacnaffscoalfdfoalndda(nCd) (cChi)tochsaitno–sgaenl–agtienlastcianffsocladf.foRledd. rRaewdnrafwronmfroefmererenfcere[1n9c5e].[1C9o5p].yCriogphyt r2i0g0h9t E20ls0e9vEielrseLvtide.r Ltd. Gelatin nanoparticles have been used for the effective delivery of a variety of Gelatin nanoparticles have been used for the effective delivery of a variety of drugs, including drugs, including polyphenols. Shutava et al. [196] encapsulated several polyphenolic polyphenols. Shutava et al. [196] encapsulated several polyphenolic compounds—epigallocatechin compounds—epigallocatechin gallate (EGCG), curcumin, tannic acid and catechin—in gelatin gallate (EGCG), curcumin, tannic acid and catechin—in gelatin nanoparticles, and modified the nanoparticles, and modified the nanoparticle surface with a layer-by-layer polyelectrolyte shell nanoparticle surface with a layer-by-layer polyelectrolyte shell to increase the stability of the gel and to increase the stability of the gel and control the release of polyphenols. The release of EGCG control the release of polyphenols. The release of EGCG from the gel was found to be up to 8 hours, from the gel was found to be up to 8 h, much longer than the minutes when in the free state. much longer than the minutes when in the free state. Furthermore, nanoparticle-coated EGCG Furthermore, nanoparticle-coated EGCG retained its biological activity in MB-MD-231 breast retained its biological activity in MB-MD-231 breast cancer cells. Karthikeyan et al. [197] prepared cancer cells. Karthikeyan et al. [197] prepared resveratrol-gelatin nanoparticles by agglomeration. resveratrol-gelatin nanoparticles by agglomeration. We understand that the nanoparticles may We understand that the nanoparticles may induce the apoptosis of cancer cells by affecting the expression induce the apoptosis of cancer cells by affecting the expression of p53, p21, caspase-3, Bax, Bcl-2 and of p53, p21, caspase-3, Bax, Bcl-2 and NF-κB. To investigate the release of free tea polyphenols and NF-κB. To investigate the release of free tea polyphenols and nanoparticulate tea polyphenols in fatty nanoparticulate tea polyphenols in fatty foods from gelatin films, chitosan nanoparticles were prepared foods from gelatin films, chitosan nanoparticles were prepared using the ionic gel method and using the ionic gel method and bonded to gelatin films. It was found that the amount of tea polyphenols bonded to gelatin films. It was found that the amount of tea polyphenols released from the gum film released from the gum film was related to the type of fatty food used and the encapsulation rate was related to the type of fatty food used and the encapsulation rate of the tea polyphenols. The of the tea polyphenols. The presence of chitosan hydrochloride increased the diffusion time of tea presence of chitosan hydrochloride increased the diffusion time of tea polyphenols in the simulant, polyphenols in the simulant, and the association was positively correlated [198]. and the association was positively correlated [198]. 3.4.3. Whey Protein (Mainly β-lactoglobulin) Nanoparticles 3.4.3. Whey Protein (Mainly β-lactoglobulin) Nanoparticles Whey protein is extracted from whey, a by-product of cheese production, and is composed of Whey protein is extracted from whey, a by-product of cheese production, and is composed of many proteins, including α-lactalbumin (α-la), β-lactoglobulin (β-lg), bovine serum albumin (BSA) many proteins, including α-lactalbumin (α-la), β-lactoglobulin (β-lg), bovine serum albumin (BSA) and immunoglobulins, and lactoferrin [199]. Whey protein is considered to be ideal for encapsulating and immunoglobulins, and lactoferrin [199]. Whey protein is considered to be ideal for encapsulating and delivering compounds such as polyphenols, due to its high safety, low cost, high nutritional value, and delivering compounds such as polyphenols, due to its high safety, low cost, high nutritional and diverse functions [200]. Among them, β-lactoglobulin is the most widely used. Beta-lactoglobulin value, and diverse functions [200]. Among them, β-lactoglobulin is the most widely used. Beta- is the main whey protein and gelling agent in milk. It is present in most mammalian milk, but not in lactoglobulin is the main whey protein and gelling agent in milk. It is present in most mammalian human milk, and is a small globular protein, consisting of only 162 amino acids, with a molecular weight milk, but not in human milk, and is a small globular protein, consisting of only 162 amino acids, with of 18.3 kDa. Whey proteins have several transfer-friendly functions, such as binding to hydrophobic a molecular weight of 18.3 kDa. Whey proteins have several transfer-friendly functions, such as active substances, gelation and emulsification. In addition, whey protein is resistant to pepsin, so it is binding to hydrophobic active substances, gelation and emulsification. In addition, whey protein is beneficial for the oral transport of polyphenols and other substances [201]. resistant to pepsin, so it is beneficial for the oral transport of polyphenols and other substances [201]. Shpigelman et al. [202] delivered EGCG with thermally modified lactoglobulin, and found that Shpigelman et al. [202] delivered EGCG with thermally modified lactoglobulin, and found that the correlation constant of EGCG with preheated protein was about 3.5 times higher than that of the the correlation constant of EGCG with preheated protein was about 3.5 times higher than that of the natural protein. Because the size of EGCG-lactoglobulin nanoparticles is relatively small, they can natural protein. Because the size of EGCG-lactoglobulin nanoparticles is relatively small, they can maintain good transparency for the processing and preparation of transparent drinks. In addition, maintain good transparency for the processing and preparation of transparent drinks. In addition, lactoglobulin encapsulation greatly protected the antioxidant activity of EGCG, and the degradation of lactoglobulin encapsulation greatly protected the antioxidant activity of EGCG, and the degradation EGCG in nanoparticles was 3.2 times slower than that of free EGCG within eight days. Li et al. [203] of EGCG in nanoparticles was 3.2 times slower than that of free EGCG within eight days. Li et al. [203] delivered curcumin with β-lactoglobulin and nanoemulsion as the carrier. The results showed that the water solubility, pH stability and permeability of curcumin were significantly improved by

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