title: Nanoencapsulation of dietary flavonoid fisetin: Formulation and in vitro antioxidant and α-glucosidase inhibition activities.
abstract: 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-(ε-caprolactone) (PCL) and PLGA-PEG-COOH, encapsulating FS were formulated as suitable oral controlled release systems. Results showed NPs having a mean diameter of 140-200nm, and a percent loading of FS ranging from 70 to 82%. In vitro release studies revealed that 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 DPPH and ABTS scavenging capacity of FS, as well as α-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 system to control the release of antioxidant and anti-hyperglycemic FS for nutraceutical and/or therapeutic application.
authors: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy; Laboratory of Nanomedicine, Department of Chemistry and Pharmacy, University of Sassari, c/o Porto Conte Ricerche, Tramariglio, 07041 Alghero, Italy.
authors: Mario
authors: M
authors: Sechi
authors: Department of Dermatology, School of Medicine and Public Health, University of Wisconsin, 1300 University Avenue, Madison, USA.
authors: Deeba N
authors: DN
authors: Syed
authors: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
authors: Nicolino
authors: N
authors: Pala
authors: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
authors: Alberto
authors: A
authors: Mariani
authors: CNR - Istituto Scienze delle Produzioni Alimentari, Traversa La Crucca, 3 - Località Baldinca, 07040 Li Punti, Sassari, Italy.
authors: Salvatore
authors: S
authors: Marceddu
authors: POLCOMING Department, Section of Information Engineering, University of Sassari, via Piandanna 4, 07100 Sassari, Italy.
authors: Antonio
authors: A
authors: Brunetti
authors: Department of Dermatology, School of Medicine and Public Health, University of Wisconsin, 1300 University Avenue, Madison, USA.
authors: Hasan
authors: H
authors: Mukhtar
authors: Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy; Laboratory of Nanomedicine, Department of Chemistry and Pharmacy, University of Sassari, c/o Porto Conte Ricerche, Tramariglio, 07041 Alghero, Italy. Electronic address: vsanna@uniss.it.
authors: Vanna
authors: V
authors: Sanna
mesh_terms: D000975:Antioxidants / Q000737:chemistry / Q000493:pharmacokinetics; D019587:Dietary Supplements; D005419:Flavonoids / Q000737:chemistry / Q000493:pharmacokinetics; D044948:Flavonols; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics; D053769:Nanocapsules / Q000737:chemistry*; D012441:Saccharomyces cerevisiae / Q000201:enzymology; D029701:Saccharomyces cerevisiae Proteins / Q000737:chemistry / Q000378:metabolism; D000520:alpha-Glucosidases / Q000737:chemistry / Q000378:metabolism
chemical_list: D000975:Antioxidants; D005419:Flavonoids; D044948:Flavonols; D065089:Glycoside Hydrolase Inhibitors; D053769:Nanocapsules; D029701:Saccharomyces cerevisiae Proteins; D000520:alpha-Glucosidases; C017875:fisetin
keywords: Antioxidant activity; Controlled release; Fisetin; Nanoparticles; α-glucosidase inhibition