Enhancement of Oral Bioavailability and Anti-hyperuricemic Activity of Isoliquiritigenin via Self-Microemulsifying Drug Delivery System

• Published in: AAPS PharmSciTech Vol. 20; no. 5; p. 218
• Main Authors: Zhang, Kangyi, Wang, Qilong, Yang, Qiuxuan, Wei, Qiuyu, Man, Na, Adu-Frimpong, Michael, Toreniyazov, Elmurat, Ji, Hao, Yu, Jiangnan, Xu, Ximing
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.07.2019
• Subjects: Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Pharmacology/Toxicology; Pharmacy; Research Article; Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery; anti-hyperuricemic; Isoliquiritigenin; ISL-SMEDDS; bioavailability; release; in vitro release
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-019-1421-0

The aim of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) for enhancement of the oral bioavailability of isoliquiritigenin (ISL) as well as evaluate its in vivo anti-hyperuricemic effect in rats. The ISL-loaded self-microemulsifying drug delivery system (ISL-SMEDDS) was comprised of ethyl oleate (EO, oil phase), Tween 80 (surfactant), and PEG 400 (co-surfactant). The ISL-SMEDDS exhibited an acceptable narrow size distribution (44.78 ± 0.35 nm), negative zeta potential (− 10.67 ± 0.86 mV), and high encapsulation efficiency (98.17 ± 0.24%). The in vitro release study indicated that the release rates of the formulation were obviously higher in different release media (HCl, pH 1.2; PBS, pH 6.8; double-distilled water, pH 7.0) compared with the ISL solution. The oral bioavailability of the ISL-SMEDDS was enhanced by 4.71 times in comparison with the free ISL solution. More importantly, ISL-SMEDDS significantly reduced uric acid level by inhibiting xanthine oxidase (XOD) activity in the model rats. Collectively, the prepared ISL-SMEDDS proved to be potential carriers for enhancing the solubility and oral bioavailability of ISL, as well as ameliorating its anti-hyperuricemic effect.