Improved Oral Absorption of Quercetin from Quercetin Phytosome®, a New Delivery System Based on Food Grade Lecithin

Abstract

Background and ObjectivesThe importance of quercetin and flavonoids in the diet and as food supplements is well known, and literature studies support their potential use to treat several human diseases. Many beneficial properties have been described for quercetin, so much effort has been directed into overcoming the major drawbacks of this natural compound—its poor solubility and low oral absorption. The aims of this study were to compare a new food-grade lecithin-based formulation of quercetin, Quercetin Phytosome®, to unformulated quercetin in terms of solubility in simulated gastrointestinal fluids and oral absorption in a randomized crossover pharmacokinetic study of healthy volunteers.MethodsThe solubility of the new formulation was determined by in vitro incubation in simulated gastrointestinal fluids, and quercetin was detected by ultra performance liquid chromatography. A single-dose, randomized, six-sequence/three-period crossover clinical trial (3 × 3 × 3 crossover design) with a balanced carryover effect was conducted in healthy volunteers under fasting conditions. Twelve healthy volunteers of both sexes with an age range of 18–50 years were recruited; one dose of quercetin and two different doses of Quercetin Phytosome were administered orally as film-coated tablets. Pharmacokinetic samples were collected at twelve time points (from 0 h to 24 h) after administration, and quercetin levels were measured by HPLC/MS/MS. Data were analyzed using the Phoenix WinNonlin (v.6.4) software package, and the most significant pharmacokinetic parameters were calculated. Statistical analysis involved performing a two-way ANOVA with repeated measures followed by post hoc analysis (Tukey’s test).ResultsSignificant improvements in both in vitro solubility and oral absorption (in terms of both exposure and maximum concentration achieved) by healthy volunteers in a human clinical study were obtained with the Quercetin Phytosome formulation as compared to unformulated quercetin.ConclusionsA more soluble formulation of quercetin based on lecithin, Quercetin Phytosome, has recently been developed, and was found to facilitate the attainment of very high plasma levels of quercetin—up to 20 times more than usually obtained following a dose of quercetin—when the novel formulation was administered orally in human volunteers, and it did not have any notable side effects. These results suggest that Quercetin Phytosome allows the oral administration of quercetin in a safe and bioavailable manner, thus facilitating the effective utilization of this natural compound to treat various human diseases.

Utilizing Liposomal Quercetin and Gallic Acid in Localized Treatment of Vaginal Candida Infections

“…This is in agreement with the reported high EE % for Q in liposomes, ranging from 67% to 89%, [56,[59][60][61]. Recently, Riva et al [41] also demonstrated that the employment of phytosomes can increase the solubility of this polyphenol, thus promoting the entrapment of Q into the vesicles.…”

“…In particular, when Q was added at the concentration of 2 mg/mL, liposomes were significantly bigger and the high PDI (>0.8) indicated the presence of precipitates. This was probably due to Q, being very poorly soluble in water, immediately precipitating when not incorporated in the lipid bilayers [41]. LP-Q prepared with the intermediate concentration (Q 1.5 mg/mL) were also excluded because of the stability issue; although equal in size to liposomes prepared with Q 1 mg/mL, they were not stable after just one week of storage at 4 • C (mean size: 504.6 ± 14.1; PDI: 0.564 ± 0.052).…”

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

“…Zhang et al [94] aimed to improve the oral absorption of baicalin, which has low solubility and poor permeability, by using a micellar formulation comprised of the carriers Pluronic P123 copolymer and sodium taurocholate. Sustained release profile of baicalin-loaded mixed micelles, in in vitro drug release experiment, held in several pH conditions, showed 14% drug released after 2 h in gastric conditions and 54% release within 48 h in intestinal conditions, compared to 34% and 79% release [105], nanoparticles [106][107][108][109][110], phytosome [111], nanoliposome [112], mixed micelles [113,114], SNEDDS [115,116], nanocarrier [117,118], nanoemulsion [119], nanosuspension [ Mixed micelles [129,130], nanoparticles [131,132], solid dispersion [133,134] , SNEDDS [135] , SMEDDS [136], lipid carrier [137], copolymeric micelles [138], exosomes [139] Naringenin DENV, HCV SNEDDS [140], solid dispersion [141], nanoparticles [142,143] , liposome [144], nanosuspension [145,146] In vitro uptake studies, carried out with a caco-2 cell line, determined the absorption of baicalin within the mixed micelles and verified their internalization ability. Baicalin-loaded ST-P123-MMs formulation achieved high oral bioavailability (Fig.…”

Healthy Protection Of Bergamot Is Linked To The Modulation Of Microbiota

“…A signi cant reduction of serum low density lipoprotein cholesterol (LDL-C) and triglyceride was also demonstrated by a new bergamot phytosome formulation [9]: in that clinical study, the delivery by phytosome allowed increased oral absorption of the naringin, the major component of bergamot, in respect to standard unformulated bergamot. Actually, phytosome techniques have recently demonstrated the successful delivering of other low-soluble natural compounds, like quercetin [20] and Coenzyme Q10 [21].…”