Nanophytosomes of hesperidin and of hesperetin: Preparation, characterization, and in vivo evaluation

Abstract

Hesperidin and hesperetin are two important plant flavanones abundantly found in citrus fruit. They have discovered many biological activities to treat diseases, including cancer, diabetes, and Alzheimer's disease. Despite their various benefits, they have poor solubility, which reduces their bioavailability and absorption. In this study, nanophytosomes have been utilized to improve their payload's solubility and bioavailability. In the current study, hesperetin or hesperidin was complexed with Phospholipon 90G with a 2:1 or 3:1 molar ratio, respectively. The formation of associations between active compounds and phospholipid were confirmed by X‐ray diffraction (XRD), Fourier‐transform infrared spectroscopy (FTIR), and nuclear magnetic resonance (NMR) techniques. Dynamic light scattering data show that the prepared associations in the presence of body fluids can make nanoparticles in the range of 200–250 nm. In addition, oral administration demonstrated that Cmax of hesperidin and hesperetin was increased (up to four times) after complexation with the lipid. It is concluded that phospholipid association may be used as a suitable and straightforward strategy to improve therapeutic activities of hesperidin and hesperetin by increasing their solubility and bioavailability.

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

“…So far, several methods have allowed us to increase this compound’s solubility and permeability. They were, for example, inclusion complex with cyclodextrin [ 24 ], phospholipid complex [ 25 ], nanoemulsions [ 26 ], nanophytosomes [ 27 ], solid dispersion [ 28 , 29 ], and nanodispersion [ 30 ]. Hesperidin delivery systems have also been confirmed with chitooligosaccharide by spray drying [ 31 ], gold nanoparticles by a chemical synthesis method [ 32 ], chitosan nanoparticles [ 33 ], and lipid–polymer hybrid nanoparticles by the emulsification solvent evaporation method [ 34 ].…”

Natural antioxidants that act against Alzheimer’s disease through modulation of the NRF2 pathway: a focus on their molecular mechanisms of action

“…In the research by Omidfar et al. ( 160 ), nanophytosomes were used to improve the solubility and bioavailability of hesperidin and hesperetin. By forming nanoparticles through the interaction of these compounds with Phospholipon 90G, their solubility was enhanced.…”

Evaluation of the cytotoxic activity of sorafenib‐loaded camel milk casein nanoparticles against hepatocarcinoma cells

“…In fact, nanocarriers have been used for the transport of nutrients, drugs, vitamins, and bioactive compounds or plant‐based products. [ 7 ] They act by enhancing the stability, solubility, and absorption in the body, thus minimizing side effects. [ 8 ] These nanocarriers can be engineered to target specific drug delivery, protect sensitive compounds from degradation and increase therapeutic efficacy.…”

“…These flavonoids show bioactivity against multiple diseases including cancer. [ 7 ] Similarly, the flavonoid, chrysin when encapsulated in nano liposomal structures alleviate the symptoms of cadmium‐induced toxicity in mice. [ 11 ] Even, Anethum graveolens nano emulsion containing carvone and limonene are suggested to be a promising strategy to protect the tissues against cadmium‐induced oxidative damage.…”