RESUMEN
A liposome of Licochalcone A (LCA-Liposomes) was purposively prepared to ameliorate the low in vivo availability and efficacy of LCA. Physical characterization of LCA-Liposomes was carried out mainly by determining particle size, morphology, zeta potential (Z-potential), and efficiency of LCA encapsulation (EE) via appropriate techniques. Also, the rate of LCA release in vitro and distribution in vivo (plasma and tissues) was evaluated. Evaluation of the antirenal activity of LCA-liposomes was carried out by establishing chronic renal failure (CRF) model in mice through intragastric administration of adenine (200 mg/kg) and subsequent determination of biochemical parameters and examination of tissue sections. Respectively, the mean size of liposomal particles, Z-potential and EE of LCA-Liposomes were 71.78 ± 0.99 nm, -38.49 ± 0.06 mV, and 97.67 ± 1.72%. Pharmacokinetic and tissue distribution studies showed that LCA-Liposomes could improve the availability of LCA in the blood and tissues, whereas during pharmacodynamics studies, the liposome effectively improved the therapeutic effect of LCA on CRF mice by potentially protecting the renal tissues while exhibiting antioxidant activity. In conclusion, LCA-Liposomes could effectively improve the bioavailability of LCA and provide platform for the development of LCA-related functional products. PRACTICAL APPLICATIONS: As a traditional Chinese medicine, licorice is widely used in food and pharmaceutical industries. LCA is a small molecule flavonoid extracted from the root of licorice. In this study, LCA was loaded on liposome carriers, which significantly improved the water solubility and oral bioavailability, and proved that LCA-Liposomes have certain therapeutic effects on chronic renal failure, thereby providing a basis for the development of LCA into drugs or functional food in the future.
Asunto(s)
Chalconas , Liposomas , Animales , Disponibilidad Biológica , Chalconas/farmacología , Liposomas/química , Ratones , SolubilidadRESUMEN
The aim of this study was to develop licochalcone A-loaded self-microemulsifying drug delivery system (LCA-SMEDDS) to improve bioavailability and anti-hyperuricemic activity of hydrophobic natural compound licochalcone A (LCA). The prepared LCA-SMEDDS was characterised by transmission electron microscopy analysis, particle size, polymer dispersity index (PDI), zeta potential, stability tests and in vitro release analysis. LCA-SMEDDS and free LCA were orally administered to Sprague-Dawley rats to investigate respective bioavailability. The hyperuricaemia rat model was established to evaluate anti-hyperuricemic activity. The particle size, PDI, and zeta potential of LCA-SMEDDS were 25.68 ± 0.79 nm, 0.074 ± 0.024, -14.37 ± 2.17 mV. The oral bioavailability of LCA-SMEDDS was increased 2.36-fold compared with the free LCA. The uric acid level of LCA-SMEDDS group (200 mg/kg) was decreased 60.08% compared with model control group. The developed LCA-SMEDDS could be an outstanding candidate for improving oral bioavailability and anti-hyperuricemic activity of LCA.