On the Development of a Cutaneous Flavonoid Delivery System: Advances and Limitations

Abstract

Flavonoids are one of the vital classes of natural polyphenolic compounds abundantly found in plants. Due to their wide range of therapeutic properties, which include antioxidant, anti-inflammatory, photoprotective, and depigmentation effects, flavonoids have been demonstrated to be promising agents in the treatment of several skin disorders. However, their lipophilic nature and poor water solubility invariably lead to limited oral bioavailability. In addition, they are rapidly degraded and metabolized in the human body, hindering their potential contribution to the prevention and treatment of many disorders. Thus, to overcome these challenges, several cutaneous delivery systems have been extensively studied. Topical drug delivery besides offering an alternative administration route also ensures a sustained release of the active compound at the desired site of action. Incorporation into lipid or polymer-based nanoparticles appears to be a highly effective approach for cutaneous delivery of flavonoids with good encapsulation potential and reduced toxicity. This review focuses on currently available formulations used to administer either topically or systemically different classes of flavonoids in the skin, highlighting their potential application as therapeutic and preventive agents.

Hesperidin-Loaded Lipid Polymer Hybrid Nanoparticles for Topical Delivery of Bioactive Drugs

“…As a topical delivery method, quercetin was loaded onto lecithin-chitosan nanoparticles. Compared to pure quercetin, the quercetin-loaded nanoparticles showed better penetration and significant deposition of quercetin in the skin [23]. The biocompatibility, hydration, hemostasis, and anti-inflammatory properties of chitosan are well known in wound therapy, where it has been approved by the FDA.…”

Selected Flavonoids to Target Melanoma: A Perspective in Nanoengineering Delivery Systems

“…Among the polyphenols, flavonoids that comprise a vast group of polyphenolic compounds with a characteristic benzo-γ-pyrone structure have important biological activities that are dependent on the degree of hydroxylation, substitutions, and conjugations of the backbone structure [ 12 ]. These compounds are easily available as nutrients in regular diets, and due to their prominent pharmaceutic potential shown in vitro and in vivo, many of these compounds are referred to as nutraceuticals [ 7 , 11 , 17 ]. In this review, five common flavonoids, namely, apigenin, epigallocatechin-3-gallate (EGCG), kaempferol, naringenin, and silybin were chosen ( Figure 2 ), and relevant studies using these compounds as anti-tumoral agents as well as strategies to improve their bioavailability and efficacy were described.…”

“…To overcome these problems, the use of nanotechnology has been suggested. Nanoparticles have a high potential to entrap and carry the desired compounds, maintain their physico-chemical stability, increase their permeabilization, help them reach the target site, and even improve their activity [ 7 , 12 , 17 ]. Currently, nanoparticles are of the highest interest, despite several constraints that science seeks to solve, aiming to improve the quality of life of people who suffer from cancer.…”

Importance of Flavonoid as Secondary Metabolites

“…They are widely used as chemotaxonomic markers and belonging to Polygonaceae, Umbelliferae, Rutaceae, Rosaceae, Leguminosae, Lamiaceae, and also Compositae. Solubility properties include soluble in water and alcohol, whereas insoluble in organic solvents [1].…”