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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, 23, x FOR PEER REVIEW 9 of 36 as the nanocarrier, enhanced the cellular uptake and ROS scavenging ability than single drug loading Molecules 2020, 25, 4613 9 of 36 [164]. Figure 3.. Liposome structure and drug loading diagram: (A) Cross-section structure of liposome, made of phospholipid and cholesterol, showing the magnifified molecular structure of a phospholipid thatconsistsofapollarheadandanon--pollarrttaiill..Phospholipidheadiishydrophobicandcomprises choline, phosphate and glycerol, while the tail is a hydrocarbon chain that shows lipophilicity. (B) A choline, phosphate and glycerol, while the tail is a hydrocarbon chain that shows lipophilicity. (B) A schematic representation of the structure and preparation of phytosomal curcumin. Reprinted from schematic representation of the structure and preparation of phytosomal curcumin. Reprinted from reference [134,159]. Copyright 2016 Elsevier Masson SAS, 2019 Elsevier Ltd. reference [134,159]. Copyright 2016 Elsevier Masson SAS, 2019 Elsevier Ltd. However, the limitation of liposome is that it has a short half-life and can be easily oxidized and However, the limitation of liposome is that it has a short half-life and can be easily oxidized and hydrolyzed. It was previously reported that the intravenous administration of resveratrol resulted in hydrolyzed. It was previously reported that the intravenous administration of resveratrol resulted in a short t1/2, ranging from 7.8 to 33 min [165]. Therefore, many modified liposomes came into being. a short t1/2, ranging from 7.8 to 33 min [165]. Therefore, many modified liposomes came into being. In In order to increase the half-life and extend the blood circulation time, Caddeo et al. [166] grafted order to increase the half-life and extend the blood circulation time, Caddeo et al. [166] grafted polyethylene glycol chains (PEGylated liposomes) at the ends of liposomes to deliver resveratrol. polyethylene glycol chains (PEGylated liposomes) at the ends of liposomes to deliver resveratrol. Drug release results indicated that the half-life of polyethylene glycol modified liposomes was increased Drug release results indicated that the half-life of polyethylene glycol modified liposomes was by about nine times, while the inherent antioxidant activity was still maintained. By mixing with increased by about nine times, while the inherent antioxidant activity was still maintained. By mixing various biopolymers, the storage stability of liposomes was improved [167]. The biopolymers include with various biopolymers, the storage stability of liposomes was improved [167]. The biopolymers anionic (such as arabinose and whey protein) and cationic (such as chitosan). It was also proven that include anionic (such as arabinose and whey protein) and cationic (such as chitosan). It was also the encapsulation rate of polyphenols in liposomes and their antioxidant activity will increase with the proven that the encapsulation rate of polyphenols in liposomes and their antioxidant activity will addition of biopolymers. increase with the addition of biopolymers. 3.2.2. Solid Lipid Nanoparticles (SLNs) 3.2.2. Solid Lipid Nanoparticles (SLNs) Solid lipid nanoparticle is a solid colloidal drug delivery system which is made by wrapping Solid lipid nanoparticle is a solid colloidal drug delivery system which is made by wrapping or or inserting drugs in lipid nucleus with natural or synthetic lipids, such as lecithin and triglyceride. inserting drugs in lipid nucleus with natural or synthetic lipids, such as lecithin and triglyceride. The The emergence and development of SLNs successfully make up for the limitations of traditional emergence and development of SLNs successfully make up for the limitations of traditional nanocarriers (such as nanoemulsion and liposomes), with advantages including controlling drug release nanocarriers (such as nanoemulsion and liposomes), with advantages including controlling drug and targeting, increasing drug stability, high drug loading, low toxicity, and loading of hydrophilic release and targeting, increasing drug stability, high drug loading, low toxicity, and loading of lipophilic drugs. hydrophilic lipophilic drugs.

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