Bioavailability of Hesperidin and Its Aglycone Hesperetin—Compounds Found in Citrus Fruits as a Parameter Conditioning the Pro-Health Potential (Neuroprotective and Antidiabetic Activity)—Mini-Review

Abstract

Hesperidin and hesperetin are polyphenols that can be found predominantly in citrus fruits. They possess a variety of pharmacological properties such as neuroprotective and antidiabetic activity. However, the bioavailability of these compounds is limited due to low solubility and restricts their use as pro-healthy agents. This paper described the limitations resulting from the low bioavailability of the presented compounds and gathered the methods aiming at its improvement. Moreover, this work reviewed studies providing pieces of evidence for neuroprotective and antidiabetic properties of hesperidin and hesperetin as well as providing a detailed look into the significance of reported modes of action in chronic diseases. On account of a well-documented pro-healthy activity, it is important to look for ways to overcome the problem of poor bioavailability.

Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases

“…Gut microbiota releases the aglycone form—hesperetin. It can be absorbed in the colon and enter the bloodstream or be further modified by the microbiota to yield short-chain fatty acids [ 14 , 15 ].…”

“…For example, Wei et al obtained amorphous hesperidin using the wetness impregnation method [ 21 , 22 ], Wdowiak et al obtained amorphous inclusion complex by solvent evaporation [ 23 ]. Nevertheless, other techniques have been widely used to improve the solubility of hesperidin [ 15 ]. So far, several methods have allowed us to increase this compound’s solubility and permeability.…”

Hesperidin enhances intestinal barrier function in Caco‐2 cell monolayers via AMPK‐mediated tight junction‐related proteins

“…Specially, in terms of industrial cost, hesperidin is economically attractive because it can be easily isolated from the waste residues from citrus fruit processing. However, hesperetin can be obtained at a high cost because of modifying process hesperidin with the use of bacterial enzymes [ 24 , 25 , 26 , 27 ]. Therefore, it is important to demonstrate the effect of glycosides of polyphenols, which have a comparative advantage in terms of price competitiveness.…”

A Comparative Study of Hesperetin, Hesperidin and Hesperidin Glucoside: Antioxidant, Anti-Inflammatory, and Antibacterial Activities In Vitro

“…Hesperidin and hesperetin have been found as major flavonoids in many plants, especially in citrus fruits [ 38 , 39 ]. Citrus fruits contain a very low amount of hesperetin (hesperidin aglycone), and most of the flavanones exist as glucosides [ 40 ].…”