Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 410, Issue 1-2, Pages 138-144Publisher
ELSEVIER
DOI: 10.1016/j.ijpharm.2011.02.064
Keywords
Puerarin; Solid lipid nanoparticles; Oral bioavailability; Pharmacokinetics; Rat; Liquid chromatography tandem mass spectrometry
Categories
Funding
- National High Technology Research and Development Program of China (863 Program) [2007AA022002]
- Guangzhou Science and Technology Bureau [2007Z3-E5051]
- Program for Innovative Academic Team in Guangzhou Education System
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Puerarin has various pharmacological effects; however, poor water-solubility and low oral bioavailability limit its clinical utility. A delivery system of solid lipid nanoparticles could enhance its oral absorption. The objective of this study was to investigate the pharmacokinetics, tissue distribution and relative bioavailability of puerarin in rats after a single dose intragastric administration of puerarin solid lipid nanoparticles (Pue-SLNs). The puerarin concentrations in plasma and tissues were determined by rapid resolution liquid chromatography electrospray ionization-tandem mass spectrometry. The C-max value of puerarin after the administration of Pue-SLNs was significantly higher than that obtained with puerarin suspension (0.33 +/- 0.05 mu g/mL vs. 0.16 +/- 0.06 mu g/mL, P < 0.01). The T-max value after the administration of the Pue-SLNs was significantly shorter than that after puerarin suspension administration (40 +/- 0 min vs. 110 +/- 15.49 min, P < 0.01). The AUC(0 -> t) values of puerarin were 0.80 +/- 0.23 mg h/L, and 2.48 +/- 0.30 mg h/L after administration of the puerarin suspension and Pue-SLNs, respectively. Following administration of the Pue-SLNs, tissue concentrations of puerarin also increased, especially in the target organs such as the heart and brain. These data suggest that SLNs are a promising delivery system to enhance the oral bioavailability of puerarin. (C) 2011 Elsevier B.V. All rights reserved.
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