Assessment of Pharmacokinetic Parameters of Daidzein-Containing Nanosuspension and Nanoemulsion Formulations After Oral Administration to Rats

大豆黄酮 生物利用度 药代动力学 最大值 化学 色谱法 药理学 口服 曲线下面积 高效液相色谱法 医学 染料木素 内分泌学
作者
Esra Demirtürk,Afife Büşra Uğur Kaplan,Meltem Çetin,Kübra Akıllıoğlu,Meltem Dönmez Kutlu,Seda Köse,Fazilet Aksu
出处
期刊:European Journal of Drug Metabolism and Pharmacokinetics [Springer Nature]
卷期号:47 (2): 247-257 被引量:10
标识
DOI:10.1007/s13318-021-00746-5
摘要

Background and ObjectivesDaidzein has several biological effects such as antioxidation, anti-inflammation, chemoprevention, and anticancer effects. The aim of this study was to evaluate the impact of nano-formulations (nanoemulsion-NE and nanosuspension-NS) prepared to increase the oral bioavailability of daidzein, a poorly water-soluble isoflavone, on the pharmacokinetic parameters of daidzein in rats. MethodsA high-performance liquid chromatography-ultraviolet (HPLC-UV) method was successfully developed for daidzein analysis in rat plasma. The pharmacokinetics studies of the nano-sized formulations, compared to coarse daidzein suspension, were carried out in the rats by a single oral dose at 10 mg/kg (n = 6/group). Area under the plasma concentration-time curve from time zero to extrapolation to time infinity (AUC0–∞), maximum plasma concentration (Cmax), time to reach maximum plasma concentration (tmax), and elimination half life (t1/2) values for coarse daidzein suspension, daidzein-NS, and daidzein-NE were estimated by a non-compartmental analysis.ResultsThe AUC values of daidzein-NE and daidzein-NS were approximately 2.62 and 2.65 times higher than that of coarse daidzein suspension, respectively (p < 0.05). Relative bioavailability (Frel) (%) values of daidzein following oral administration of nanosuspension or nanoemulsion formulations were about 265.6% and 262.3%, respectively.ConclusionIt revealed that nanoscale size is an important factor to overcome any dissolution rate barriers to oral bioavailability of the low water-soluble compound. Nanoemulsion and nanosuspension formulations are beneficial dosage forms to increase the oral bioavailability of Biopharmaceutical Classification System (BCS) Class II and Class IV compounds.
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