4.5 Article

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

Journal

JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 110, Issue 6, Pages 2555-2561

Publisher

ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2021.02.030

Keywords

Nanodrug; Intestinal absorption; Hesperetin; Bioavailability; Pharmacokinetics

Funding

  1. National Natural Science Foundation of China (NSFC) [21974015]

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By preparing a nanoemulsion vehicle, the oral bioavailability of hesperetin was significantly improved, with a notable increase in lymphatic transport and absorption in the intestine.
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.& nbsp; (c) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.

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