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Int J Nanomedicine ; 13: 4133-4144, 2018.
Article in English | MEDLINE | ID: mdl-30038494

ABSTRACT

BACKGROUND: Resveratrol (RES) is a natural anti-inflammatory and antioxidant compound with poor water solubility and oral bioavailability. The present study takes the advantages of nanocarriers combined with a ligand (galactose) anchoring to orally deliver RES in an attempt to improve its bioavailability and pharmacological activity. METHODS: RES-loaded galactosylated nanoparticles (RES-GNPs) were prepared by solvent diffusion technique using poly(lactic-co-glycolic acid), synthesized N-oleoyl-d-galactosamine and Tween 80. RES-GNPs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Oral bioavailability and in vitro anti-inflammatory activity were investigated in rats and lipopolysaccharides-induced RAW 264.7 cells, respectively. RESULTS: The resulting RES-GNPs were 108.4 nm around in particle size with a polydispersity index of 0.217. Furthermore, RES-GNPs possessed a high EE and a slow drug release in water. After oral administration, RES-GNPs significantly enhanced the oral bioavailability of RES, up to 335.7% relative to RES suspensions. In situ single-pass intestinal perfusion and cellular uptake experiments showed that GNPs could improve the intestinal permeability and transcellular transport of RES. Moreover, the anti-inflammatory efficacy of RES-GNPs in RAW 264.7 cells model was superior to free RES and RES-GNPs. CONCLUSION: The results indicate that RES-GNPs can effectively promote the intestinal absorption of RES and strengthen its bioactivity, which may be a promising system for the treatment of inflammatory diseases.


Subject(s)
Anti-Inflammatory Agents/therapeutic use , Galactosamine/chemistry , Inflammation/drug therapy , Lactic Acid/chemistry , Nanoparticles/chemistry , Polyglycolic Acid/chemistry , Stilbenes/administration & dosage , Stilbenes/therapeutic use , Administration, Oral , Animals , Anti-Inflammatory Agents/pharmacology , Biological Availability , Caco-2 Cells , Drug Liberation , Endocytosis/drug effects , Galactosamine/chemical synthesis , Humans , Inflammation/blood , Inflammation/pathology , Intestinal Absorption , Intestinal Mucosa/metabolism , Male , Nanoparticles/administration & dosage , Nanoparticles/ultrastructure , Particle Size , Permeability , Polylactic Acid-Polyglycolic Acid Copolymer , Proton Magnetic Resonance Spectroscopy , Rats, Sprague-Dawley , Resveratrol , Solubility , Stilbenes/blood , Stilbenes/pharmacokinetics
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