| Background: Resveratrol effects on the prevention and treatment of colon
cancer have been well documented recently, but low solubility, rapid
absorption and metabolism of resveratrol limit its beneficial effects on colon
cancer. Designing a formulation that enhances the solubility of resveratrol,
protects resveratrol from oxidation and isomerization, and delivers it to the
colon is a priority of food and drug industry. In this study, resveratrolpolyethylene
glycol (PEG)-loaded pectin-chitosan polyelectrolyte complex
was designed as a colon targeted delivery system.
Methods: The effects of adding PEG, ultra-sonication time, pH, and pectin to
chitosan ratio were investigated on particle size, polydispersity index (PDI),
zeta potential by particle size analyzer, and scanning electron microscopy
(SEM). Encapsulation efficiency (EE), release of resveratrol in simulated
gastrointestinal fluid, and different pHs were analyzed via High Performance
Liquid Chromatography (HPLC). Antioxidant activity was measured by (2, 2-
diphenyl-1-picryl-hydrazyl-hydrate) DPPH free-radical method.
Results: Results showed that colloidal stable micro-particles (725 ± 20 nm)
with PDI < 0.3 and zeta potential +27 ± 2 mV was formed in the ratio of 5:1
of pectin to chitosan w/v % after a 10-min sonication. Encapsulation
efficiency was 81 ± 7 %. The reduction of antioxidant activity of resveratrol
loaded micro-particles after one month was less than 13%. Micro-particles
released about 33% of resveratrol in the simulated gastric and intestinal fluids.
Conclusion: Two-thirds of the loaded resveratrol in Pectin-Chitosan complex
reached colon. The developed system had enough specification for enriching
fruit based drinks due to remarkable colloidal stability in the pH range of 3.5
to 4.5. |