In vitro release and pharmacokinetics of quercetin-loaded mixed micelles composed of Pluronic P123/Poloxamer 188 in rats / 中国药理学通报

ABSTRACT

Aim: To investigate the in vitro release behavior and pharmacokinetic characteristics of quercetinloaded mixed micelles composed of Pluronic P123/ Poloxamer 188 in rats. Methods: Polymer micelles were prepared by the thin-film hydration method. The quercetin release rate of quercetin mixed micelles was investigated by dynamic membrane dialysis technique in the physiological saline contained 1% Tween-80. The drug release curves were drawn. The results were evaluated by DD Solver. Ultra performance liquid chromatography (UPLC) method was employed to measure the plasma concentration of quercetin in rats after tail intravenous administration. The plasma concentration-time curves were drawn, and the pharmacokinetic parameters were calculated with PK Solver. Results: The entrapment efficiency (EE%) and loading efficiency (DL%) of mixed micelles was (94. 25 ± 2. 13)% and (8.61 ± 0. 18)%, respectively. The quercetin release rate of quercetin mixed micelles in the physiological saline contained 1% Tween-80 was (52.90 ± 1.08)%. The quercetin mixed micelles could be described by Higuchi model and expressed by the equation; F = 6. 735 t0.5 (Rsqr-adj = 0. 960 4, AlC = 75. 584 0). T1/2β, AUC0.4 and MRT0-inf of quercetin mixed micelles were calculated to be 1.2,1.5 and 2. 4 times of free quercetin, respectively. Conclusions: The quercetin-loaded mixed micelles have high entrapment efficiency and loading efficiency, which can improve the release behavior in vitro, prolong the time of quercetin, and significantly enhance the fraction of bioavailability of quercetin in rats.