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Int J Pharm. 2016 Mar 30;501(1-2):342-9. doi: 10.1016/j.ijpharm.2016.01.081. Epub 2016 Feb 6.

Enhanced oral bioavailability and in vivo antioxidant activity of chlorogenic acid via liposomal formulation.

Author information

1
Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
2
Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China. Electronic address: yjn@ujs.edu.cn.
3
Center for Nano Drug/Gene Delivery and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang 212013, China. Electronic address: xmxu@ujs.edu.cn.

Abstract

In the present study, a formulation system consisting of cholesterol and phosphatidyl choline was used to prepare an effective chlorogenic acid-loaded liposome (CAL) with an improved oral bioavailability and an increased antioxidant activity. The developed liposomal formulation produced regular, spherical and multilamellar-shaped distribution nanoparticles. The pharmacokinetic analysis of CAL compared with chlorogenic acid (CA), showed a higher value of Cmax(6.42 ± 1.49 min versus 3.97 ± 0.39 min) and a delayed Tmax(15 min versus 10 min), with 1.29-fold increase in relative oral bioavailability. The tissue distribution in mice also demonstrated that CAL predominantly accumulated in the liver which indicated hepatic targeting potential of the drug. The increased activities of antioxidant enzymes (Total Superoxide Dismutase (T-SOD) and Glutathione Peroxidase (GSH-Px)) and total antioxidant capacity (T-AOC), in addition to decreased level of malondialdehyde (MDA) in CCl4-induced hepatotoxicity study further revealed that CAL exhibited significant hepatoprotective and antioxidant effects. Collectively, these findings present a liposomal formulation with significantly improved oral bioavailability and an increased in vivo antioxidant activity of CA.

KEYWORDS:

Antioxidant activity; Bioavailability; Chlorogenic acid; Hepatoprotective; Liposome

PMID:
26861689
DOI:
10.1016/j.ijpharm.2016.01.081
[Indexed for MEDLINE]

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