title: Characterization of trans-resveratrol-loaded lipid-core nanocapsules and tissue distribution studies in rats.
abstract: Several studies have reported that orally ingested trans-resveratrol is extensively metabolized in the enterocyte before it enters the blood and target organs. Additionally, trans-resveratrol is photosensitive, easily oxidized and presents unfavorable pharmacokinetics. Therefore, it is of great interest to stabilize trans-resveratrol in order to preserve its biological activities and to improve its bioavailability in the brain. Here, trans-resveratrol was loaded into lipid-core nanocapsules and analyzed for particle size, polydispersity and zeta potential. The nanocapsule distribution in brain tissue was evaluated by intraperitoneal (i.p.) and gavage routes in healthy rats. The lipid-core nanocapsules had a mean diameter of 241 nm, a polydispersity index of 0.2, and a zeta potential of -15 mV. No physical changes were observed after 1, 2 and 3 months of storage at 25 degrees C. Lipid-core nanocapsules showed high entrapment of trans-resveratrol and displayed a higher trans-resveratrol concentration in the brain, the liver and the kidney after daily i.p. or gavage administration than that observed for the free trans-resveratrol. Because trans-resveratrol is a potent cyclooxygenase-1 inhibitor, gastrointestinal damage was evaluated. The animals that were administered with trans-resveratrol-loaded lipid-core nanocapsules showed significantly less damage when compared to those administered with free trans-resveratrol. In summary, lipid-core nanocapsules exhibited great trans-resveratrol encapsulation efficiency. trans-Resveratrol-loaded lipid-core nanocapsules increased the concentration of trans-resveratrol in the brain tissue. Gastrointestinal safety was improved when compared with free trans-resveratrol. Thus, trans-resveratrol-loaded lipid-core nanocapsules may be used as an alternative potential therapeutic for several diseases including Alzheimer's disease.
authors.affiliation: Departamento de Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, 90035-003, RS, Brazil.
authors.forename: Rudimar L
authors.initials: RL
authors.lastname: Frozza
authors.forename: Andressa
authors.initials: A
authors.lastname: Bernardi
authors.forename: Karina
authors.initials: K
authors.lastname: Paese
authors.forename: Juliana B
authors.initials: JB
authors.lastname: Hoppe
authors.forename: Thaline
authors.initials: T
authors.lastname: da Silva
authors.forename: Ana M O
authors.initials: AM
authors.lastname: Battastini
authors.forename: Adriana R
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: Silvia S
authors.initials: SS
authors.lastname: Guterres
authors.forename: Christianne
authors.initials: C
authors.lastname: Salbego
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000493:pharmacokinetics* / Q000494:pharmacology; D004355:Drug Stability; D041981:Gastrointestinal Tract / Q000187:drug effects; D006863:Hydrogen-Ion Concentration; D008055:Lipids / Q000737:chemistry; D008297:Male; D053769:Nanocapsules / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D000077185:Resveratrol; D013267:Stilbenes / Q000493:pharmacokinetics* / Q000494:pharmacology
chemical_list: D000975:Antioxidants; D008055:Lipids; D053769:Nanocapsules; D013267:Stilbenes; D000077185:Resveratrol