Pharmacokinetics, tissue distribution and relative bioavailability of puerarin solid lipid nanoparticles following oral administration.

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 μg/mL vs. 0.16±0.06 μg/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.

Luo CF ，Yuan M ，Chen MS ，Liu SM ，Zhu L ，Huang BY ，Liu XW ，Xiong W ... -  《-》

[Pharmacokinetics and bioavailability of Puerarin self-microemulsion in Beagle dogs].

Chen XX ，Yuan S ，Li G ，Liang YY ，Zhou X ，Xie CS ，Long CF ... -  《-》

Formulation optimization and bioavailability after oral and nasal administration in rabbits of puerarin-loaded microemulsion.

The main objective of the study was to investigate the efficacy of microemulsion (ME) to facilitate bioavailability of puerarin (PUE) after oral and nasal administration. The pseudo-ternary phase diagrams were constructed to screen the ME components and optimize the ME formulation. The optimized formulation for bioavailability assessment consisted of 20% Tween 80, 20% glycerin, and 1.6% ethyl oleate. The solubility (27.8 mg/mL) of PUE in ME was significantly improved compared to that (4.58 mg/mL) of crude PUE in water. The ME droplets were spherical with a mean particle diameter of 23.4 nm. After nasal (5 mg/kg) and oral (20 mg/kg) administration of a single dose of PUE as ME to fasted rabbits, the absolute bioavailability was 34.58% and 13.54%, respectively. It showed a shorter T(max) (0.75 h) for nasal administration than that (1.0 h) for oral administration of PUE-loaded ME. The C(max) of PUE-loaded ME was 0.55 μg/mL after nasal administration and 0.64 μg/mL after oral administration, respectively. The results showed that nasal administration might be a promising route to enhance the absorption of PUE in the form of ME.

Yu A ，Wang H ，Wang J ，Cao F ，Gao Y ，Cui J ，Zhai G ... -  《-》

Metabolic profile of puerarin in rats after intragastric administration of puerarin solid lipid nanoparticles.

Luo CF ，Hou N ，Tian J ，Yuan M ，Liu SM ，Xiong LG ，Luo JD ，Chen MS ... -  《International Journal of Nanomedicine》

Formulation optimization of self-emulsifying preparations of puerarin through self-emulsifying performances evaluation in vitro and pharmacokinetic studies in vivo.

Quan DQ ，Xu GX 《-》