Hasija, R.
Assessment of polymeric nanoparticles to enhance oral bioavailability and antioxidant activity of resveratrol - Vol.83(6), Nov-Dec - Mumbai Indian Journal of Pharmaceutical Science 2021 - 1114-1128p.
Resveratrol has proven as potential natural antioxidant, non-flavonoid polyphenolic compound, but it has
limitations such as low water solubility, which substantially restricts oral bioavailability. To enhance oral
bioavailability and antioxidant potential of resveratrol by fabricating the resveratrol encapsulated oral
eudragit® E100 based polymeric nano-delivery system. Resveratrol-encapsulated polymeric nanoparticles
were developed by solvent extraction and diffusion method. Copolymer, eudragit® E100 polymeric
matrices were used to prepared polymeric nanoparticles and in vitro physicochemically characterized.
Furthermore, in vivo pharmacokinetic and antioxidant potential of optimized resveratrol-encapsulated
polymeric nanoparticles was evaluated. The resveratrol-encapsulated polymeric nanoparticles exhibited
optimum mean particle size (410±9.78 nm), polydispersity index (0.203±0.079) and encapsulation
efficiency (66.88±5.45 %), respectively. In vitro release profile of resveratrol showed >25 % release in first
2 h in phosphate-buffered saline pH 7.4 followed by >75 % at the end of 48 h. The optimized resveratrol-
encapsulated polymeric nanoparticles were stable at the accelerated condition and room temperature,
respectively. The optimized resveratrol-encapsulated polymeric nanoparticles demonstrated significantly
higher oral bioavailability (~4.07-fold; p<0.05) as compared to pure resveratrol. Furthermore, the
optimized resveratrol-encapsulated polymeric nanoparticles were evaluated for free radical scavenging
activity and showed to increase the activity with time i.e. after 72 h, it was the same as pure resveratrol but
at 24 h no increase in antioxidant activity was observed with optimized resveratrol-encapsulated polymeric
nanoparticles. Furthermore, half-maximal inhibitory concentration of the optimized resveratrol-
encapsulated polymeric nanoparticles was decreased with time. Results are suggesting that resveratrol-
encapsulated polymeric nanoparticles are the promising approach using eudragit® E100 as a polymeric
material to enhance oral bioavailability and antioxidant potential of insoluble resveratrol.
PHARMACEUTICS
Assessment of polymeric nanoparticles to enhance oral bioavailability and antioxidant activity of resveratrol - Vol.83(6), Nov-Dec - Mumbai Indian Journal of Pharmaceutical Science 2021 - 1114-1128p.
Resveratrol has proven as potential natural antioxidant, non-flavonoid polyphenolic compound, but it has
limitations such as low water solubility, which substantially restricts oral bioavailability. To enhance oral
bioavailability and antioxidant potential of resveratrol by fabricating the resveratrol encapsulated oral
eudragit® E100 based polymeric nano-delivery system. Resveratrol-encapsulated polymeric nanoparticles
were developed by solvent extraction and diffusion method. Copolymer, eudragit® E100 polymeric
matrices were used to prepared polymeric nanoparticles and in vitro physicochemically characterized.
Furthermore, in vivo pharmacokinetic and antioxidant potential of optimized resveratrol-encapsulated
polymeric nanoparticles was evaluated. The resveratrol-encapsulated polymeric nanoparticles exhibited
optimum mean particle size (410±9.78 nm), polydispersity index (0.203±0.079) and encapsulation
efficiency (66.88±5.45 %), respectively. In vitro release profile of resveratrol showed >25 % release in first
2 h in phosphate-buffered saline pH 7.4 followed by >75 % at the end of 48 h. The optimized resveratrol-
encapsulated polymeric nanoparticles were stable at the accelerated condition and room temperature,
respectively. The optimized resveratrol-encapsulated polymeric nanoparticles demonstrated significantly
higher oral bioavailability (~4.07-fold; p<0.05) as compared to pure resveratrol. Furthermore, the
optimized resveratrol-encapsulated polymeric nanoparticles were evaluated for free radical scavenging
activity and showed to increase the activity with time i.e. after 72 h, it was the same as pure resveratrol but
at 24 h no increase in antioxidant activity was observed with optimized resveratrol-encapsulated polymeric
nanoparticles. Furthermore, half-maximal inhibitory concentration of the optimized resveratrol-
encapsulated polymeric nanoparticles was decreased with time. Results are suggesting that resveratrol-
encapsulated polymeric nanoparticles are the promising approach using eudragit® E100 as a polymeric
material to enhance oral bioavailability and antioxidant potential of insoluble resveratrol.
PHARMACEUTICS