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

J Pharm Sci. 2021 Jun;110(6):2555-2561. doi: 10.1016/j.xphs.2021.02.030. Epub 2021 Feb 27.

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 AUC0-t and Cmax 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.

Keywords: Bioavailability; Hesperetin; Intestinal absorption; Nanodrug; Pharmacokinetics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Emulsions
  • Hesperidin
  • Intestinal Absorption*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Emulsions
  • Hesperidin
  • hesperetin