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. 2012 Sep;13(3):961-6.
doi: 10.1208/s12249-012-9819-y. Epub 2012 Jun 30.

An excellent delivery system for improving the oral bioavailability of natural vitamin E in rats

Yinhua Gong  1 , Yunkai Wu, Chunli Zheng, Liya Fan, Fei Xiong, Jiabi Zhu
Affiliations

An excellent delivery system for improving the oral bioavailability of natural vitamin E in rats

Yinhua Gong et al. AAPS PharmSciTech. 2012 Sep.

Abstract

This study set out to develop a novel and stable nanoemulsion formulation of natural vitamin E with increased oral bioavailability. The natural vitamin E nanoemulsion was prepared by a modified emulsification technique. The physicochemical characteristics of natural vitamin E nanoemulsion were characterized and its pharmacokinetics study was performed as well. The experimental results showed droplet diameters ranging from 20 to 400 nm (average, 87.7 nm) with a negative electrostatic potential (-23.5 ± 1.5 mv). The pharmacokinetics study of this nanoemulsion and corresponding soft capsule was carried out using noncompartment model method. Compared with the marketed soft capsule, the C (max) of the natural vitamin E nanoemulsion was higher, while the T (max) was shorter. Thus, plasma concentration-time profiles in rats dosed with nanoemulsion showed a 1.6-fold enhancement in the area under the curve of natural vitamin E compared with the marketed soft capsule. The antioxidative effects of the natural vitamin E nanoemulsion and the marketed soft capsule were also evaluated by the levels of superoxide dismutase (SOD) activity and malondialdehyde (MDA) concentration in serum and liver tissue. According to the SOD activity and the MDA concentration determined, the nanoemulsion was superior to the marketed soft as an antioxidative agent. The overall results demonstrated that the nanoemulsion drug delivery system could be a promising strategy for the delivery of natural vitamin E, which showed great potential for clinical application.

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Figures

Fig. 1
Fig. 1
Size distribution of natural vitamin E nanoemulsion
Fig. 2
Fig. 2
TEM image of natural vitamin E nanoemulsion. Bar 200 nm
Fig. 3
Fig. 3
Increase in plasma concentration of natural vitamin E after single oral administration of nanoemulsion formulation and soft capsule (n = 5)
Fig. 4
Fig. 4
The activity of SOD in blood serum and liver tissue. *p < 0.1, **p < 0.05 compared with soft capsule group; #p < 0.05, ##p < 0.01 compared with the model group
See this image and copyright information in PMC

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