Improving
the Effectiveness of (−)-Epigallocatechin
Gallate (EGCG) against Rabbit Atherosclerosis by EGCG-Loaded Nanoparticles
Prepared from Chitosan and Polyaspartic Acid
posted on 2014-12-31, 00:00authored byZhiyong Hong, Yongquan Xu, Jun-Feng Yin, Jianchang Jin, Yongwen Jiang, Qizhen Du
(−)-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.