Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay

Abstract

Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl 4 )-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl 4 intoxication and to carry out an antioxidant effect.Pharmaceutics 2020, 12, 143 2 of 18 and anticancer activities [1][2][3]. These intrinsic properties, together with their biocompatibility and remarkable antioxidant activity, have attracted researchers' attention to explore potential therapeutic applications [4,5].Quercetin (3, 30, 4, 5, 7-pentahydroxyflavone) is probably the most studied bioflavonoid, belonging to the family of flavonols; its therapeutic applications include hepatoprotection [6], prevention of neural cell apoptosis [7] and cancer chemo-prevention and treatment [8].Quercetin acts as strong antioxidant by scavenging free radicals and transition metal ions, thus decreasing the process of lipid peroxidation, which is responsible for the development of many diseases, e.g., cardiovascular and neurodegenerative diseases, as well as liver damage [9][10][11].However, quercetin therapeutic applications present challenges due to (i) low aqueous solubility, (ii) photo and oxidative degradability, (iii) high first-pass effect, (iv) poor intestinal absorption and, hence, low systemic...

NIR Stimulus-Responsive PdPt Bimetallic Nanoparticles for Drug Delivery and Chemo-Photothermal Therapy

“…Moreover, H&E-stained slices of heart, liver, spleen, lung, kidney and brain displayed no obvious tissue damage occurred in these organs of mice receiving different treatments ( Figure 7 ). The levels of ALT and AST in serum of mice were further determined for the indication of hepatotoxicity [ 46 ]. Mice received PdPt@HA or DOX@PdPt@HA NPs injection showed similar levels of ALT and AST in serum compared with the control group ( P > 0.05), suggesting a favorable safety profile of the PdPt bimetallic NPs.…”

Microwave-Assisted One-Pot Lipid Extraction and Glycolipid Production from Oleaginous Yeast Saitozyma podzolica in Sugar Alcohol-Based Media

“…Thus, by using such a biomass, short-chained glycolipids could be formed. The production of laurate sugar esters raises interest, especially in the pharmaceutical industry where they are notably used to form drug delivery systems [ 52 , 53 ]. The properties of the glycolipids can be influenced not only by chain length but also by the ramifications and degree of unsaturation [ 54 , 55 ].…”

Prunus spinosa Extract Loaded in Biomimetic Nanoparticles Evokes In Vitro Anti-Inflammatory and Wound Healing Activities

“…6, 9, 17-24) that are known as wound-healing modulators [41]. Furthermore, molecules highly loaded into PSF-DOPCs such as caffeic acid and quercetin derivatives (quercetin xyloside) have already been explored in the literature showing an antioxidant [42] and anti-inflammatory effect through downregulation of the TLR-4 signaling pathway [43,44]. On this basis, our findings seem to confirm that these are the components of the PSF extract most directly involved in determining the observed experimental results.…”

“…The object of the present work is to evaluate and characterize the effective incorporation of the active molecules present in PSF from both a qualitative and a quantitative standpoint and to evaluate the ability of the formulations to reduce the inflammation process and improve the wound-healing repair. 42.291" (350 m above sea level) and, immediately after harvesting, frozen and stored at −20 • C until use. For the extraction, 50 g of fruit pulp were homogenized in an Osterizer for 3 min in 50 mL of 70% acidified aqueous ethanol solution (70 mL ethanol/29.9 mL distilled H 2 O/0.1 mL HCl 36%).…”