title: Preparation and characterization of fenofibrate-loaded nanostructured lipid carriers for oral bioavailability enhancement.
abstract: The aim of this study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of a lipid lowering agent, fenofibrate (FEN). FEN-loaded NLCs (FEN-NLCs) were prepared by hot homogenization followed by an ultrasonication method using Compritol 888 ATO as a solid lipid, Labrafil M 1944CS as a liquid lipid, and soya lecithin and Tween 80 as emulsifiers. NLCs were characterized in terms of particle size and zeta potential, surface morphology, encapsulation efficiency, and physical state properties. Bioavailability studies were carried out in rats by oral administration of FEN-NLC. NLCs exhibited a spherical shape with a small particle size (84.9 ± 4.9 nm). The drug entrapment efficiency was 99% with a loading capacity of 9.93 ± 0.01% (w/w). Biphasic drug release manner with a burst release initially, followed by prolonged release was depicted for in vitro drug release studies. After oral administration of the FEN-NLC, drug concentration in plasma and AUCt-∞ was fourfold higher, respectively, compared to the free FEN suspension. According to these results, FEN-NLC could be a potential delivery system for improvement of loading capacity and control of drug release, thus prolonging drug action time in the body and enhancing the bioavailability.
authors.affiliation: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyeongsan, 712-749, South Korea.
authors.forename: Tuan Hiep
authors.initials: TH
authors.lastname: Tran
authors.forename: Thiruganesh
authors.initials: T
authors.lastname: Ramasamy
authors.forename: Duy Hieu
authors.initials: DH
authors.lastname: Truong
authors.forename: Han-Gon
authors.initials: HG
authors.lastname: Choi
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers; D045703:Emulsifying Agents / Q000737:chemistry; D005227:Fatty Acids / Q000737:chemistry*; D011345:Fenofibrate / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*; D005989:Glycerides / Q000737:chemistry*; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*; D054709:Lecithins / Q000737:chemistry; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D014465:Ultrasonics
chemical_list: D004337:Drug Carriers; D045703:Emulsifying Agents; D005227:Fatty Acids; D005989:Glycerides; D000960:Hypolipidemic Agents; C514708:Labrafil M 1944 CS; D054709:Lecithins; D011136:Polysorbates; C086409:glyceryl behenate; D011092:Polyethylene Glycols; D011345:Fenofibrate