Nanoencapsulation of dietary flavonoid fisetin: Formulation and in vitro antioxidant and ?-glucosidase inhibition activities

The bioactive flavonoid fisetin (FS) is a diet-derived antioxidant that is being increasingly investigated for its health-promoting effects. Unfortunately, the poor physicochemical and pharmacokinetic properties affect and limit the clinical application. In this study, novel polymeric nanoparticles (NPs), based on Poly-(?-caprolactone) (PCL) and PLGA-PEG-COOH, encapsulating FS were formulated as suitable oral controlled release systems. Results showed NPs having a mean diameter of 140-200 nm, and a percent loading of FS ranging from70 to 82%. In vitro release studies revealedthat NPs are able to protect and preserve the release of FS in gastric simulated conditions, also controlling the release in the intestinal medium. Moreover, the DPPHand ABTS scavenging capacity of FS, as well as ?-glucosidase inhibition activity, that resulted about 20-fold higher than commercial Acarbose, were retained during nanoencapsulation process. In summary, our developed NPs can be proposed as an attractive delivery systemto control the release of antioxidant and anti-hyperglycemic FS for nutraceutical and/or therapeutic application.