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BACKGROUND 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). METHODS: 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. RESULTS: 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). CONCLUSIONS: 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. [ABSTRACT FROM AUTHOR]

Liquiritin, as one of the main flavonoids in Glycyrrhiza, exhibits extensive pharmacological effects, such as the anti-oxidant, anti-inflammatory, anti-tumor and so on. Herein, the aqueous solubility and oral bioavailability of liquiritin was purposely enhanced via the preparation of the mixed micelles. The liquiritin-loaded micelles (LLM) were fabricated via thin-film dispersion method. The optimal LLM formulation was evaluated through physical properties including particle size (PS), encapsulation efficiency (EE) and drug loading (DL). In vitro accumulate release as well as in vivo pharmacokinetics were also evaluated. Moreover, the hypolipidemic activity of LLM was observed in the hyperlipidemia mice model. The LLM exhibited a homogenous spherical shape with small mean PS, good stability and high encapsulation efficiency. The accumulate release rates in vitro of the LLM were obviously higher than free liquiritin. The oral bioavailability of the formulation was heightened by 3.98 times in comparison with the free liquiritin. More importantly, LLM increased the hypolipidemic and effect of alleviating lipid metabolism disorder in hepatocytes of liquiritin in hyperlipidemia mice model. Collectively, the improved solubility of liquiritin in water coupled with its enhanced oral bioavailability and concomitant hypolipidemic activity could be attributed to the incorporation of the drug into the mixed micelles. [ABSTRACT FROM AUTHOR]

The pharmacological activities of liquiritin (LT) are greatly limited by its insolubility and low oral absorption. The purpose of this study was to prepare LT-hydroxypropyl-beta-cyclodextrin inclusion complex (LT-HP-β-CD) to increase water solubility, oral bioavailability and antitumor effect of LT. Herein, saturated aqueous solution method was applied to prepare the LT-HP-β-CD prior to characterization via scanning electron microscope (SEM), infrared radiation (IR) spectroscopy, X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC). Also, in vitro release and in vivo pharmacokinetics were evaluated. Moreover, the anti-tumor activity of the formulation was investigated in the A549 lung cancer cells. The results of SEM, IR, XRD and DSC showed that LT-HP-β-CD was successfully formulated. In vitro release and oral bioavailability of LT-HP-β-CD compared with the free LT was significantly higher. Successfully, antitumor effect of LT was remarkably enhanced by the preparation of LT-HP-β-CD. Altogether, the LT-HP-β-CD represents a potential carrier for enhancing the water solubility and oral bioavailability of LT coupled with antitumor activity enhancement. [Display omitted] [ABSTRACT FROM AUTHOR]

The purpose of this study was to develop a precursor liposome nano-delivery system for liquiritin (LT) to improve its solubility, oral bioavailability, and efficacy. The characterizations of the particle diameter, zeta potential, polydispersity index (PDI), droplet morphology, drug release in vitro , and oral bioavailability of the prepared LT precursor liposomes (LTMs) were carried out. In addition, streptozotocin intraperitoneal injection successfully induced diabetic mouse model, while the LT hypoglycemic effect, oral glucose tolerance, biochemical parameters and pathological sections were studied. The prepared LTMs were diluted to obtain a clear and transparent solution with a diameter of 91.84 ± 1.85 nm, zeta potential of −38.59 ± 2.65 mV and PDI of 0.215 ± 0.016. The in vitro release of the LTMs was superior to that of the free LT suspension, which may be related to the increased solubility of LT, as well as the small diameter and increased surface area. The obtained pharmacokinetic parameters indicated that the relative oral bioavailability of LTMs was increased by 8.8 times compared with the free LT suspension. Pharmacodynamic studies showed that LTMs effectively improved LT's hypoglycemic effect and diabetes-related organ repair, simultaneously confirmed its antioxidant activity. These results implied that the LTMs was an effective method to improve the solubility, oral bioavailability, and hypoglycemic activity of LT. [ABSTRACT FROM AUTHOR]