Fabrication of Luteolin Nanoemulsion by Box-Behnken Design to Enhance its Oral Absorption Via Lymphatic Transport.

AAPS PharmSciTech

National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Chinese Medicine, Nanchang, 330006, People's Republic of China.

Published: September 2024

AI Article Synopsis

  • Intestinal lymphatic transport is a promising method for drug delivery that bypasses first-pass metabolism, improving oral bioavailability and aiding lymphoid-related diseases treatment.
  • Luteolin (LUT), despite its potential, struggles with poor water solubility and low bioavailability, but using nanoemulsion can enhance its delivery, as explored through Box-Behnken design optimization.
  • The study found that luteolin nanoemulsions (LUT NEs) had increased stability and significant improvements in oral bioavailability, with a 3.5-fold enhancement in permeability and nearly tripled bioavailability when compared to LUT suspension, confirming their effectiveness in promoting lymphatic transport.

Article Abstract

Intestinal lymphatic transport offers an alternative and effective way to deliver drugs, such as avoiding first-pass metabolism, enhancing oral bioavailability, and facilitating the treatment of targeted lymphoid-related diseases. However, the clinical use of luteolin (LUT) is limited by its poor water solubility and low bioavailability, and enhancing lymphatic transport by nanoemulsion may be an efficient way to enhance its oral bioavailability. The objective of this work is to prepare the luteolin nanoemulsions (LUT NEs), optimized its preparation parameters by using Box-Behnken design optimization (BBD) and evaluated it in vitro and in vivo. An Caco-2 / Raji B cell co-incubation monolayer model was established to simulate the M-cell pathway, and the differences in the transmembrane transport of LUT and NEs were compared. Cycloheximide (CHX) was utilized to establish rat chylomicron (CM) blocking model, and for investigating the influence of pharmacokinetic parameters in rats thereafter. The results showed that LUT NEs have good stability, the particle sizes were about 23.87 ± 0.57 nm. Compared with LUT suspension, The P of LUT NEs was enhanced for 3.5-folds, the oral bioavailability was increased by about 2.97-folds. In addition, after binding with chylomicron, the oral bioavailability of LUT NEs was decreased for about 30% (AUC (μg/L*h): 5.356 ± 1.144 vs 3.753 ± 0.188). These results demonstrated that NEs could enhance the oral absorption of luteolin via lymphatic transport routes.

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Source
http://dx.doi.org/10.1208/s12249-024-02898-4DOI Listing

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