Nanoemulsion for Improving the Oral Bioavailability of Hesperetin: Formulation Optimization and Absorption Mechanism

Abstract

This study aimed to prepare a nanoemulsion vehicle to improve the oral bioavailability of hesperetin. The pseudo-ternary phase diagrams and the RSM were used to optimize nanoemulsion parameters. Compared with hesperetin suspension, the AUC 0-t and C max of nanoemulsion were increased by 5.67-fold and 2.64-fold, respectively. The proportion of lymphatic transport reached 87.72%, the cumulative absorption amount of jejunum, ileum, and duodenum increased by 1.1-fold, 1.92-fold, and 1.5-fold, respectively. The results implied that hesperetin nanoemulsion could effectively improve the bioavailability of hesperetin by increasing lymphatic transport and enhancing intestinal permeability. Therefore, nanoemulsion is a potential method to improve the bioavailability of hesperetin, which has strong practicability.

Amorphous Inclusion Complexes: Molecular Interactions of Hesperidin and Hesperetin with HP-Β-CD and Their Biological Effects

“…Saad et al managed to produce solid lipid nanoparticles of Hed, which translated into nearly 4.5-fold higher bioavailability in the rat model [ 25 ]. Zeng et al generated the nanoemulsion of Het, which improved oral bioavailability by 5.67-fold in terms of AUC [ 57 ]. Gu Su-Fang et al obtained the D-α-tocopheryl polyethylene glycol 1000 succinate micelles and phosphatidylcholine complexes with Het, which translated into 16.2- and 18.0-fold increased AUC of plasma concentration after oral administration [ 58 ].…”

Development of a naringenin microemulsion as a prospective ophthalmic delivery system for the treatment of corneal neovascularization: in vitro and in vivo evaluation

“…The equation showed that an increase in oil weight ( A ) resulted in an increase in DS and a decrease in DL. According to the relevant literature, the stability of MEs is related to the DS of the emulsion, which means that a smaller DS can avoid aggregation and precipitation and thus result in better stability (Zeng et al., 2021 ). The characteristics of small DS and PDI, high DL and EE can also enhance the permeability.…”

“…Distilled water was added dropwise to a mixture of oil and S/Cos (Km) under gentle magnetic stirring at 37 °C until the mixture became clear at a certain point (Kassaee & Mahboobian, 2021 ; Zeng et al., 2021 ). The system with low viscosity and a clear appearance was considered to be a microemulsion.…”

Nanoemulsion delivery systems for enhanced efficacy of antimicrobials and essential oils

“…NE are usually employed to enhance the stability and bioavailability of lipophilic antimicrobials and can increase a drug's oral bioavailability in gastrointestinal (GI) fluids and their capability of crossing the epithelial layer of the intestine. Multiple mechanisms can contribute to the bioavailability enhancement effect of NE including increasing drug solubility and stability, 54 enhancing drug intestinal permeability, 16,55 increasing drug lymphatic transport, 56 and decreasing/preventing the drug efflux via the efflux transporters in the GI tract. 57,58 Upon oral administration, NE are inevitably diluted in the GI fluids and are subject to the GI microenvironment (Fig.…”