Pharmacokinetics, tissue distribution and relative bioavailability of puerarin solid lipid nanoparticles following oral administration
Pharmacokinetics, tissue distribution and relative bioavailability of puerarin solid lipid nanoparticles following oral administration
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DOI：
10.1016/j.ijpharm.2011.02.064
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发表时间：
2011-05-30
影响因子：
5.8
通讯作者：
Xiong, Wen
中科院分区：
文献类型：
--
作者：
Luo, Cheng-Feng;Yuan, Mu;Xiong, Wen
葛根素具有多种药理作用，但水溶性差和口服生物利用度低限制了其临床应用。固体脂质纳米粒给药系统可促进其口服吸收。研究葛根素固体脂质纳米粒（Pue-SLNs）单次灌胃给药后在大鼠体内的药代动力学、组织分布和相对生物利用度。采用快速分辨液相色谱-电喷雾串联质谱法测定血浆和组织中葛根素的浓度。Pue-SLN给药后葛根素的C-max值显著高于葛根素混悬液给药后的C-max值（0.33 +/- 0.05 μ g/mL vs. 0.16 +/- 0.06 μ g/mL，P < 0.01）。Pue-SLN给药后的Tmax值明显短于葛根素混悬液给药后的Tmax值（40 ± 0 min vs. 110 ± 15.49 min，P < 0.01）。葛根素混悬液和Pue-SLN给药后，葛根素的AUC（0 -> t）值分别为0.80 +/- 0.23 mg h/L和2.48 +/- 0.30 mg h/L。Pue-SLN给药后，葛根素的组织浓度也增加，特别是在靶器官如心脏和大脑中。这些数据表明，SLN是一个有前途的传递系统，以提高葛根素的口服生物利用度。(C)2011 Elsevier B. V.保留所有权利。
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.