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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 8 of 36 separate the internal and external aqueous medium [14,153] (Figure 3). Liposomes vary in size, ranging from 50 nm to 1 μm, depending on composition and preparation methods. The presence of such an amphiphilic substance allows water-soluble, fat-soluble and amphiphilic compounds to be encapsulated, transferred and released [154]. Table 3. Polyphenols complexed with phospholipids. Phytosomal Formulations Moringa oleifera leaf phytophospholipid complex Quercetin phytosome Curcumin phytosome Rutin-phospholipid Catechin phyto-phospholipid Luteolin phytosome Silybin phospholipid EGCG phytosome Grape seed phytosome Quercetin phytosome Silybin phytosome Persimmon phytosome Route of Administration In vitro Oral [139] Biological Activity Wound healing Antimicrobial, anti-infammatory, anticancer Antioxidant Anticytotoxicity, neuroprotection Antioxidant Hepatoprotective Hepatoprotective, antioxidant, anticancer Anticancer Anticancer Antioxidant, anti-inflammatory Hepatoprotective Antioxidant Reference In vitro, oral In vitro [141,142] [143] [144] In vitro Oral [145] In vivo Oral Oral Oral Oral Oral [140,146] [147] [148] [149] [150] [151] [138] There are many methods for preparing liposomes. The traditional methods include thin film hydration, reverse evaporation, injection, and heating [155]. The biggest drawback of these technologies is that the liposomes formed are large in size. The methods currently used include membrane contactor-based method, freeze drying of double emulsion method, proliposome method [156]. With the ability to improve biocompatibility, prevent drug degradation, deliver low-solubility drugs, and improve drug targeting [157–159], liposomes are undoubtedly a kind of promising and flexible polyphenol delivery system. In addition, it has been recognized in clinical and biological research for its role in human health, including protecting the liver, enhancing memory and reducing cholesterol intake [152]. With the deep understanding of liposomes and polyphenols, the combination of liposomes and polyphenols has attracted much attention. Cheng reported that nano-liposomes greatly improved the bioavailability and water solubility of curcumin [160]. Vanaja et al. [161] used a thin-film method to load resveratrol into liposomes. Compared with free resveratrol, resveratrol packed in liposomes was more active in cells in vivo and had more significant antioxidant effect. A novel remote loading approach using chemically modified β-cyclodextrin was applied to incorporate curcumin into liposomes [162]. The results proved that the encapsulation of the nanoparticles significantly improved the bioavailability of curcumin, and the complexation of cyclodextrin further increased the encapsulation efficiency of curcumin. Huang and coworkers co-loaded curcumin and resveratrol in liposomes [163]. Infrared spectroscopy and fluorescence techniques demonstrated that curcumin was connected to the hydrophobic acyl chain region of liposomes, while resveratrol was located in the polar hydrophilic region. The study also investigated the physical and chemical properties of the liposomes. The results showed that, when the ratio of curcumin to resveratrol was 5:1, the encapsulation rate and the antioxidant activity was the highest. Similarly, co-loading quercetin and resveratrol, using liposome as the nanocarrier, enhanced the cellular uptake and ROS scavenging ability than single drug loading [164].

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