期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 394, 期 1-2, 页码 179-185出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2010.05.005
关键词
Nanostructure lipid carriers; Vinpocetine; Oral bioavailability; Sustained release; Poorly water-soluble drugs
资金
- National Ministry of Science and Technology, China [2009CB930300]
The purpose of this study is to develop an optimized nanostructured lipid carriers (NLC) formulation for vinpocetine (VIN), and to estimate the potential of NLC as oral delivery system for poorly water-soluble drug. In this work, VIN-loaded NLC (VIN-NLC) was prepared by a high pressure homogenization method. The VIN-NLC showed spherical morphology with smooth surface under transmission electron microscope (TEM) and scanning electron microscopic (SEM) analysis. The average encapsulation efficiency was 94.9 +/- 0.4%. The crystallization of drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC). The drug was in an amorphous state in the NLC matrix. In the in vitro release study, VIN-NLC showed a sustained release profile of VIN and no obviously burst release was observed. The oral bioavailability study of VIN was carried out using Wistar rats. The relative bioavailability of VIN-NLC was 322% compared with VIN suspension. In conclusion, the NLC formulation remarkably improved the oral bioavailability of VIN and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. (C) 2010 Elsevier B.V. All rights reserved.
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