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Improving the effectiveness of (-)-epigallocatechin gallate (EGCG) against rabbit atherosclerosis by EGCG-loaded nanoparticles prepared from chitosan and polyaspartic acid.

Abstract
(-)-Epigallocatechin gallate (EGCG) is the major bioactive compound in green tea. Its effect is limited by the harsh environment of the gastrointestinal tract. The present study investigates how the effectiveness of EGCG is influenced by its encapsulation into self-assembled nanoparticles of chitosan (CS) and aspartic acid (PAA). Blank nanoparticles with a mean diameter of ca. 93 nm were prepared from 30-50 kDa PAA and 3-5 kDa CS with a mass rate of 1:1. EGCG was loaded in the nanoparticles to yield EGCG-CS-PAA nanoparticles with an average diameter of 102 nm, which were pH-responsive and demonstrated different EGCG release profiles in simulated gastrointestinal tract media. The average ratio (%) of lipid deposition for EGCG-CS-PAA nanoparticles administered orally to rabbits was 16.9 ± 5.8%, which was close to that of oral simvastatin (15.6 ± 4.1%). Orally administered EGCG alone yielded an average ratio of lipid deposit area of 42.1 ± 4.0%, whereas this value was 65.3 ± 10.8% for the blank nanoparticles. The effectiveness of EGCG against rabbit atherosclerosis was significantly improved by incorporating EGCG into the nanoformulation.
AuthorsZhiyong Hong, Yongquan Xu, Jun-Feng Yin, Jianchang Jin, Yongwen Jiang, Qizhen Du
JournalJournal of agricultural and food chemistry (J Agric Food Chem) Vol. 62 Issue 52 Pg. 12603-9 (Dec 31 2014) ISSN: 1520-5118 [Electronic] United States
PMID25483592 (Publication Type: Evaluation Studies, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Drug Carriers
  • Peptides
  • polyaspartate
  • Catechin
  • Chitosan
  • epigallocatechin gallate
Topics
  • Animals
  • Atherosclerosis (drug therapy)
  • Biological Availability
  • Catechin (administration & dosage, analogs & derivatives, chemistry)
  • Chemistry, Pharmaceutical (methods)
  • Chitosan (chemistry)
  • Drug Carriers (chemistry)
  • Drug Delivery Systems
  • Humans
  • Male
  • Nanoparticles (chemistry)
  • Particle Size
  • Peptides (chemistry)
  • Rabbits

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