title: Enhancing Topical Delivery of Resveratrol through a Nanosizing Approach.
abstract: Resveratrol is a naturally occurring polyphenol with strong antioxidant and free radical scavenging properties, recently proposed as a therapeutic agent for skin diseases. In this study, we investigated the possibility of improving the dermal bioavailability of the poorly water-soluble drug resveratrol by nanocrystal technology. To this purpose, nanosuspensions were prepared by the wet media milling technique, using Poloxamer 188 or Tween 80 as stabilizers, and characterized by means of both solid state and morphological and dimensional studies. All analytical data demonstrated that neither a modification of the drug crystalline pattern nor the isomerization of thetransdouble bond were observed after the wet media milling particle size reduction process, which produced rounded and smooth nanocrystals with a mean diameter ranging between 0.2-0.3 µm. Resveratrol skin delivery from nanosuspension formulations was evaluated by the pig ear skin model via tape stripping. Results of the experiments showed that after application of nanosuspension formulations, higher amounts of resveratrol could penetrate the skin at deeper levels compared to drug coarse suspensions. The antioxidant activity of resveratrol in nanocrystals was assessed by the DPPH assay, which demonstrated that the size reduction process as well as the formulation compositions did not modify the drug antioxidant activity.
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Sinico
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Rosa
authors.initials: R
authors.lastname: Pireddu
authors.affiliation: Dept. Scienze Farmaceutiche, Sezione di Chimica Generale e Organica "A. Marchesini", University of Milan, Milan, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Pini
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Valenti
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Caddeo
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
authors.affiliation: Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Cagliari, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Lai
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage*; D001682:Biological Availability; D016503:Drug Delivery Systems; D066298:In Vitro Techniques; D053758:Nanoparticles; D010316:Particle Size; D000077185:Resveratrol; D012869:Skin Absorption; D013267:Stilbenes / Q000008:administration & dosage*; D013552:Swine
chemical_list: D000975:Antioxidants; D013267:Stilbenes; D000077185:Resveratrol