Pharm Sci. 2017;23(1):42-49 doi: 10.15171/PS.2017.07
A Colon Targeted Delivery System for
Resveratrol Enriching in pH Responsive-Model
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, resveratrol-polyethylene glycol (PEG)-loaded
pectin-chitosan polyelectrolyte complex was designed as a colon targeted
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.