Literature DB >> 33440781

Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying.

Eun-Sol Ha1, Du Hyung Choi2, In-Hwan Baek3, Heejun Park4, Min-Soo Kim1.   

Abstract

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

Entities:  

Keywords:  bioavailability; resveratrol; solid dispersion; solubility

Year:  2021        PMID: 33440781      PMCID: PMC7828062          DOI: 10.3390/antiox10010090

Source DB:  PubMed          Journal:  Antioxidants (Basel)        ISSN: 2076-3921


  32 in total

1.  Aminoalkyl methacrylate copolymers for improving the solubility of tacrolimus. I: Evaluation of solid dispersion formulations.

Authors:  Takatsune Yoshida; Ippei Kurimoto; Keiichi Yoshihara; Hiroyuki Umejima; Naoki Ito; Shunsuke Watanabe; Kazuhiro Sako; Akihiko Kikuchi
Journal:  Int J Pharm       Date:  2012-03-03       Impact factor: 5.875

2.  Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach.

Authors:  Sang Yeob Park; Zion Kang; Prakash Thapa; Yong Suk Jin; Joo Won Park; Hye Jung Lim; Jae Young Lee; Sa-Won Lee; Min-Hyo Seo; Min-Soo Kim; Seong Hoon Jeong
Journal:  Int J Pharm       Date:  2019-05-25       Impact factor: 5.875

Review 3.  Bioavailability of resveratrol.

Authors:  Thomas Walle
Journal:  Ann N Y Acad Sci       Date:  2011-01       Impact factor: 5.691

Review 4.  The bioavailability and distribution of trans-resveratrol are constrained by ABC transporters.

Authors:  Joana M Planas; Irene Alfaras; Helena Colom; M Emília Juan
Journal:  Arch Biochem Biophys       Date:  2012-06-26       Impact factor: 4.013

5.  Effect of aminoalkyl methacrylate copolymer E/HCl on in vivo absorption of poorly water-soluble drug.

Authors:  Takatsune Yoshida; Ippei Kurimoto; Keiichi Yoshihara; Hiroyuki Umejima; Naoki Ito; Shunsuke Watanabe; Kazuhiro Sako; Akihiko Kikuchi
Journal:  Drug Dev Ind Pharm       Date:  2012-10-15       Impact factor: 3.225

6.  Optimization of trans-Resveratrol bioavailability for human therapy.

Authors:  Marie Josephe Amiot; Beatrice Romier; Thi-Mai Anh Dao; Raphaelle Fanciullino; Joseph Ciccolini; Remy Burcelin; Laurent Pechere; Claude Emond; Jean-François Savouret; Eric Seree
Journal:  Biochimie       Date:  2013-01-31       Impact factor: 4.079

7.  Metabolism and disposition of resveratrol in rats: extent of absorption, glucuronidation, and enterohepatic recirculation evidenced by a linked-rat model.

Authors:  Jean-Francois Marier; Pascal Vachon; Ari Gritsas; Jie Zhang; Jean-Pierre Moreau; Murray P Ducharme
Journal:  J Pharmacol Exp Ther       Date:  2002-07       Impact factor: 4.030

Review 8.  Clinical Application of Antioxidants to Improve Human Oocyte Mitochondrial Function: A Review.

Authors:  Cristina Rodríguez-Varela; Elena Labarta
Journal:  Antioxidants (Basel)       Date:  2020-11-28

9.  The therapeutic potential of resveratrol: a review of clinical trials.

Authors:  Adi Y Berman; Rachel A Motechin; Maia Y Wiesenfeld; Marina K Holz
Journal:  NPJ Precis Oncol       Date:  2017-09-25

10.  Pure Trans-Resveratrol Nanoparticles Prepared by A Supercritical Antisolvent Process Using Alcohol and Dichloromethane Mixtures: Effect of Particle Size on Dissolution and Bioavailability in Rats.

Authors:  Eun-Sol Ha; Heejun Park; Seon-Kwang Lee; Woo-Yong Sim; Ji-Su Jeong; In-Hwan Baek; Min-Soo Kim
Journal:  Antioxidants (Basel)       Date:  2020-04-22
View more
  1 in total

Review 1.  Drug Delivery Strategies for Curcumin and Other Natural Nrf2 Modulators of Oxidative Stress-Related Diseases.

Authors:  Nina Katarina Grilc; Matej Sova; Julijana Kristl
Journal:  Pharmaceutics       Date:  2021-12-12       Impact factor: 6.321

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.