Preparation and Characterization of Fenofibrate-Loaded Nanostructured Lipid Carriers for Oral Bioavailability Enhancement

作者：Tuan Hiep Tran; Ramasamy Thiruganesh; Duy Hieu Truong; Choi Han Gon; Yong Chul Soon^*; Kim Jong Oh

来源：AAPS PHARMSCITECH, 2014, 15(6): 1509-1515.

DOI：10.1208/s12249-014-0175-y

• bioavailability
• fenofibrate
• nanoparticles
• nanostructured lipid carriers

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 pote\ntial, 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-8 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.

• 出版日期2014-12