Enhanced oral bioavailability and anti‐hyperuricemic activity of liquiritin via a self‐nanoemulsifying drug delivery system

生物利用度 化学 药理学 赋形剂 色谱法 溶解度 Zeta电位 药品 药物输送 甘草苷 高效液相色谱法 材料科学 有机化学 纳米技术 医学 纳米颗粒
作者
Chunmei Wei,Qilong Wang,Wen Weng,Michael Adu‐Frimpong,Elmurat Toreniyazov,Hao Ji,Ximing Xu,Jiangnan Yu
出处
期刊:Journal of the Science of Food and Agriculture [Wiley]
卷期号:102 (5): 2032-2040 被引量:5
标识
DOI:10.1002/jsfa.11542
摘要

This study focused on the development of a self-nanoemulsifying drug delivery system (SNEDDS) to improve, potentially, the solubility and oral bioavailability of liquiritin (LQ).The solubility of LQ in different types of excipient, namely oils (OLs), emulsifiers (EMs), and co-emulsifiers (CO-EMs), was evaluated, and a pseudo-ternary phase diagram (PTPD) and the formulation optimization were established. The prepared self-nanoemulsifying drug delivery system of liquiritin (LQ-SNEDDS) was assessed using droplet size (DS), zeta potential (ZP), polydispersity index (PDI), droplet morphology, drug release in vitro, and oral bioavailability.After the dilution of the LQ-SNEDDS, a transparent nanoemulsion was obtained with an acceptable DS (24.70 ± 0.73 nm), ZP (-18.69 ± 1.44 mV), and PDI (0.122 ± 0.006). The LQ-SNEDDS that was developed had a better release rate in vitro than the free LQ suspension. Pharmacokinetic evaluation showed that the relative oral bioavailability of LQ-SNEDDS was increased by 5.53 times, and LQ-SNEDDS exhibited a delayed half life and longer retention time in comparison with those of free LQ. Similarly, LQ-SNEDDS had a better urate lowering effect and provided better organ protection than free LQ at the same dose (P < 0.05).The incorporation of LQ into SNEDDS could serve as a promising approach to improve the solubility, oral bioavailability, and anti-hyperuricemic effect of LQ. © 2021 Society of Chemical Industry.
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