Assessment of Polymeric Nanoparticles to Enhance Oral Bioavailability and Antioxidant Activity of Resveratrol

Abstract

Resveratrol has proven potential natural antioxidant, non-flavanoid 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 (Resveratrol-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 -polymeric nanoparticles was evaluated. The Resveratrol -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-polymeric nanoparticles stable at the accelerated condition and room temperature, respectively. The optimized resveratrol-polymeric nanoparticles demonstrated significantly higher oral bioavailability (~4.07-fold; p<0.05) as compared to pure resveratrol. Furthermore, the optimized resveratrol-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-polymeric nanoparticles. Furthermore, half-maximal inhibitory concentration of the optimized resveratrol-polymeric nanoparticles was decreased with time. Resveratrol results are suggesting that resveratrol-polymeric nanoparticles are the promising approach using eudragit® E100 as a polymeric material to enhance oral bioavailability and antioxidant potential of insoluble resveratrol.