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

被引:110
|
作者
Tuan Hiep Tran [1 ]
Ramasamy, Thiruganesh [1 ]
Duy Hieu Truong [1 ]
Choi, Han-Gon [2 ]
Yong, Chul Soon [1 ]
Kim, Jong Oh [1 ]
机构
[1] Yeungnam Univ, Coll Pharm, Gyongsan 712749, South Korea
[2] Hanyang Univ, Coll Pharm, Ansan 426791, South Korea
来源
AAPS PHARMSCITECH | 2014年 / 15卷 / 06期
基金
新加坡国家研究基金会;
关键词
bioavailability; fenofibrate; nanoparticles; nanostructured lipid carriers; DRUG-DELIVERY SYSTEM; VIVO EVALUATION; NANOPARTICLES; OPTIMIZATION; NANOCRYSTALS; DISSOLUTION; DESIGN; SMEDDS; ACID; SLN;
D O I
10.1208/s12249-014-0175-y
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:1509 / 1515
页数:7
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