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Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

Authors Jingling, Na, Ji H, Hongmei, Zhiyong, Wu L

Published 19 October 2011 Volume 2011:6 Pages 2429—2435


Review by Single-blind

Peer reviewer comments 3

Jingling Tang2, Na Xu1,2, Hongyu Ji1, Hongmei Liu1, Zhiyong Wang1, Linhua Wu1,2
1Department of Pharmacy, the Second Affiliated Hospital of Harbin Medical University, Key Laboratory of College in Heilongjiang Province; 2Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, China

Background: Genistein, one of the major isoflavones, has received great attention as a phytoestrogen and potential cancer chemoprevention agent. However, the dissolution and bioavailability of genistein from solid oral preparations is low due to its poor water solubility.
Methods: In order to improve the oral bioavailability of genistein, genistein nanoparticles were prepared by the nanoprecipitation technique using Eudragit® E100 as carriers and an optimized formulation of mass ratio (genistein:Eudragit E100, 1:10). The mean particle size of genistein nanoparticles was approximately 120 nm when diluted 100 times with distilled water. The drug-loaded nanoparticles were spherical on observation by transmission electric microscopy.
Results: Encapsulation efficiency and drug loading of the genistein nanoparticles were approximately 50.61% and 5.02%, respectively. Release of drug from the genistein nanoparticles was two times greater than that from the conventional capsules. After administration of genistein suspension or genistein nanoparticles at a single dose of 100 mg/kg to fasted rats, the relative bioavailability of genistein from the nanoparticles compared with the reference suspension was 241.8%.
Conclusion: These results suggested that a nanoparticle system is a potentially promising formulation for the efficient delivery of poorly water-soluble drugs by oral administration.

Keywords: bioavailability, dissolution, genistein, nanoparticles, nanoprecipitation technique

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