The role of lipid-based nano delivery systems on oral bioavailability enhancement of fenofibrate, a BCS II drug: comparison with fast-release formulations

Journal of Nanobiotechnology

Research

Kaili Hu¹  Yi Lu²  Zhiqiang Tian²  Jianping Qi²  Wei Wu²  Kai Wang³  Tengfei Weng³  Zongning Yin⁴ 

[1] Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, 201203, Shanghai, PR China;School of Pharmacy, Key Laboratory of Smart Drug Delivery of Ministry of Education, Fudan University, 201203, Shanghai, PR China;School of Pharmacy, Key Laboratory of Smart Drug Delivery of Ministry of Education, Fudan University, 201203, Shanghai, PR China;West China School of Pharmacy, Sichuan University, 610041, Chengdu, Sichuan, PR China;West China School of Pharmacy, Sichuan University, 610041, Chengdu, Sichuan, PR China;

关键词: Fenofibrate;    Solid dispersion;    Nanostructured lipid carrier;    Self-microemulsifying drug delivery system;    Bioavailability;   

DOI  :  10.1186/s12951-014-0039-3

 received in 2014-08-13, accepted in 2014-09-13,  发布年份 2014

来源: Springer

【 摘 要 】

The aim of this study was to compare various formulations solid dispersion pellets (SDP), nanostructured lipid carriers (NLCs) and a self-microemulsifying drug delivery system (SMEDDS) generally accepted to be the most efficient drug delivery systems for BCS II drugs using fenofibrate (FNB) as a model drug. The size and morphology of NLCs and SMEDDS was characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Their release behaviors were investigated in medium with or without pancreatic lipase. The oral bioavailability of the various formulations was compared in beagle dogs using commercial Lipanthyl® capsules (micronized formulation) as a reference. The release of FNB from SDP was much faster than that from NLCs and SMEDDS in medium without lipase, whereas the release rate from NLCs and SMEDDS was increased after adding pancreatic lipase into the release medium. However, NLCs and SMEDDS increased the bioavailability of FNB to 705.11% and 809.10%, respectively, in comparison with Lipanthyl® capsules, although the relative bioavailability of FNB was only 366.05% after administration of SDPs. Thus, lipid-based drug delivery systems (such as NLCs and SMEDDS) may have more advantages than immediate release systems (such as SDPs and Lipanthyl® capsules).

【 授权许可】

Unknown   
© Weng et al.; licensee BioMed Central Ltd. 2014. This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.