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

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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 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-∞ 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.

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Acknowledgments

This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Ministry of Education, Science and Technology (No. 2012R1A2A2A02044997 and No. 2012R1A1A1039059).

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Authors and Affiliations

  1. College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyeongsan, 712-749, South Korea

    Tuan Hiep Tran, Thiruganesh Ramasamy, Duy Hieu Truong, Chul Soon Yong & Jong Oh Kim

  2. College of Pharmacy, Hanyang University, 55, Hanyangdaehak-ro, Sangnok-gu, Ansan, 426-791, South Korea

    Han-Gon Choi

Authors
  1. Tuan Hiep Tran
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  2. Thiruganesh Ramasamy
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  3. Duy Hieu Truong
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  4. Han-Gon Choi
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  5. Chul Soon Yong
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  6. Jong Oh Kim
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Correspondence to Chul Soon Yong or Jong Oh Kim.

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Tran, T.H., Ramasamy, T., Truong, D.H. et al. Preparation and Characterization of Fenofibrate-Loaded Nanostructured Lipid Carriers for Oral Bioavailability Enhancement. AAPS PharmSciTech 15, 1509–1515 (2014). https://doi.org/10.1208/s12249-014-0175-y

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  • DOI: https://doi.org/10.1208/s12249-014-0175-y

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