Impact of Quercetin Encapsulation with Added Phytosterols on Bilayer Membrane and Photothermal-Alteration of Novel Mixed Soy Lecithin-Based Liposome

Abstract

This study used highly lipophilic agents with an aim to increase the oxidant inhibitory activity and enhance photothermal stability of a novel mixed soy lecithin (ML)-based liposome by changing the composition of formulation within the membrane. Specifically, the development and optimization of the liposome intended for improving Trolox equivalent antioxidant capacity (TEAC) value and %TEAC loss was carried out by incorporating a natural antioxidant, quercetin (QU). In this context, a focus was set on QU encapsulation in ML-based liposomes and the concentration-dependent solubility of QU was investigated and calculated as encapsulation efficiency (EE). To explore the combined effects of the incorporation of plant sterols on the integrity and entrapment capacity of mixed phospholipid vesicles, conjugation of two types of phytosterols (PSs), namely β-sitosterol (βS) and stigmasterol (ST), to mixed membranes at different ratios was also performed. The EE measurement revealed that QU could be efficiently encapsulated in the stable ML-based liposome using 0.15 and 0.1 g/100 mL of βS and ST, respectively. The aforementioned liposome complex exhibited a considerable TEAC (197.23%) and enhanced TEAC loss (30.81%) when exposed to ultraviolet (UV) light (280–320 nm) over a 6 h duration. It appeared that the presence and type of PSs affect the membrane-integration characteristics as well as photodamage transformation of the ML-based liposome. The association of QU with either βS or ST in the formulation was justified by their synergistic effects on the enhancement of the EE of liposomes. Parallel to this, it was demonstrated that synergistic PS effects could be in effect in the maintenance of membrane order of the ML-based liposome. The findings presented in this study provided useful information for the development and production of stable QU-loaded ML-based liposomes for food and nutraceutical applications and could serve as a potential mixed lipids-based delivery system in the disease management using antioxidant therapy.

Quercetin‐encapsulated magnetoliposomes: Fabrication, optimization, characterization, and antioxidant studies

“…[8][9][10] In order to increase the solubility and bioavailability of QU, these constraints are thought to be solved by strategically incorporating it into a stable nanocarrier system, such as cubosomes, [11] gold nanoparticles, [12] iron nanoparticles, [13] nanocapsule, [14] nanodiamonds, [15] nanogel, [16] nanosponges, [17] niosomes, [18] phytosomes, [19] silver nanoparticles, [20] solid-lipid nanoparticles, [21] nanosuspension, [22] inclusion complexes, [23] prodrugs, [24] nanoemulsions, [25] and liposomes (LPs). [26] Loading QU into LPs can improve the aqueous solubility, stability, bioavailability, intracellular uptake, and even blood circulation time while reducing undesirable toxicity and side effects. [27] Currently, lipid-based carrier systems have gained huge attention in targeted drug delivery concerning their good biocompatibility and enhanced bioavailability of lipophilic molecules.…”

Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin

“…Nonetheless, QT exhibits poor dissolution behavior due to its low solubility that is only 0.01 mg·mL −1 in water at 25 °C [ 10 ], which seriously limited its oral bioavailability. In the past few decades, considerable research efforts have been devoted to enhancing the solubility of QT in water, thus improving its oral bioavailability, such as liposomes [ 11 ], self-microemulsion [ 12 ], and nanocrystals [ 13 , 14 , 15 ]). But these methods still have some limitations such as poor stability and low drug loading capacity.…”

Production and characterization of newly developed alcohol-free topical liposome-gel transdermal drug delivery systems containing estradiol (E2)/ estriol (E3) for post-menopausal women

“…The characteristic band of HSPC is seen at 1690 cm −1 corresponding to C=O stretching vibration, and absorbance maxima are seen around 2922 and 2862 cm −1 due to the C-H bands [30]. The cholesterol spectrum has a characteristic weak broadband at 3180-3450 cm −1 corresponding to O-H stretch [31].…”