Enhanced oral bioavailability and anti-hyperuricemic activity of liquiritin via a self-nanoemulsifying drug delivery system.
J Sci Food Agric
; 102(5): 2032-2040, 2022 Mar 30.
Article
en En
| MEDLINE
| ID: mdl-34558068
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.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Sistemas de Liberación de Medicamentos
/
Nanopartículas
Idioma:
En
Revista:
J Sci Food Agric
Año:
2022
Tipo del documento:
Article
Pais de publicación:
Reino Unido