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Review
. 2023 Jun 5;15(6):1656.
doi: 10.3390/pharmaceutics15061656.

Recent Advances in Nanoformulations for Quercetin Delivery

Ekaterina-Michaela Tomou  1 , Paraskevi Papakyriakopoulou  2 , Elmina-Marina Saitani  2 , Georgia Valsami  2 , Natassa Pippa  2 , Helen Skaltsa  1
Affiliations
Review

Recent Advances in Nanoformulations for Quercetin Delivery

Ekaterina-Michaela Tomou et al. Pharmaceutics. .

Abstract

Quercetin (QUE) is a flavonol that has recently received great attention from the research community due to its important pharmacological properties. However, QUE's low solubility and extended first-pass metabolism limit its oral administration. This review aims to present the potential of various nanoformulations in the development of QUE dosage forms for bioavailability enhancement. Advanced drug delivery nanosystems can be used for more efficient encapsulation, targeting, and controlled release of QUE. An overview of the primary nanosystem categories, formulation processes, and characterization techniques are described. In particular, lipid-based nanocarriers, such as liposomes, nanostructured-lipid carries, and solid-lipid nanoparticles, are widely used to improve QUE's oral absorption and targeting, increase its antioxidant activity, and ensure sustained release. Moreover, polymer-based nanocarriers exhibit unique properties for the improvement of the Absorption, Distribution, Metabolism, Excretion, and Toxicology (ADME(T)) profile. Namely, micelles and hydrogels composed of natural or synthetic polymers have been applied in QUE formulations. Furthermore, cyclodextrin, niosomes, and nanoemulsions are proposed as formulation alternatives for administration via different routes. This comprehensive review provides insight into the role of advanced drug delivery nanosystems for the formulation and delivery of QUE.

Keywords: anti-inflammatory; antioxidant; drug-delivery systems; nanoformulations; quercetin.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Illustration of nanoparticles’ (NP) applications in the field of pharmaceuticals.
Figure 2
Figure 2
Illustration of QUE-delivery nanosystems. The chemical structure of QUE was designed using the ChemDraw® v.16.0 software.
Figure 3
Figure 3
QUE biosynthetic pathway (ChemDraw® v.16.0 software). (a) Schematic biosynthesis mechanism from L-phenylalanine to the flavanone, naringenin. Naringenin structure is marked with a yellow colour box. (b) Schematic biosynthesis mechanism from naringenin to QUE. Its structure is marked with an orange colour box. Abbreviations of the involved catalytic enzymes are shown.
Figure 3
Figure 3
QUE biosynthetic pathway (ChemDraw® v.16.0 software). (a) Schematic biosynthesis mechanism from L-phenylalanine to the flavanone, naringenin. Naringenin structure is marked with a yellow colour box. (b) Schematic biosynthesis mechanism from naringenin to QUE. Its structure is marked with an orange colour box. Abbreviations of the involved catalytic enzymes are shown.
Figure 4
Figure 4
Schematic illustration of encapsulation of QUE-poly(n-butylcyanoacrylate) NPs by emulsion polymerization. Adopted from Bagad and Khan (2015) [61].
Figure 5
Figure 5
Schematic representation of nanoparticles functionalization with RVG29 peptide (not drawn to scale). DSPE-PEG-MAL is a 1,2-distearoyl-sn-glycero-3- phosphoethanolamine (DSPE) associated with polyethylene glycol (PEG) and terminal maleimide groups (MAL). The maleimide groups can react with thiol groups, thereby forming thioether bonds. Adopted by Pinheiro et al. (2020) [96].
Figure 6
Figure 6
(a) Appearance of empty niosomes and quercetin-niosomes; (b) Transmission electron microscopy (TEM) image of blank niosomes; (c) TEM image of quercetin-niosomes. Adopted from Lu et al. (2019) [119].
See this image and copyright information in PMC

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