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SMEDDS for improved oral bioavailability and anti-hyperuricemic activity of licochalcone A

Zhongan ZhuDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, ChinaJing LiuDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, ChinaYuhang YangDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, ChinaMichael Adu‐FrimpongHao JiElmurat ToreniyazovJiangsu Provincial Research Center for Medicinal Function Development of New Food Resources, Zhenjiang, ChinaQilong WangDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, ChinaJiangnan YuDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, ChinaXiming XuDepartment of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, Jiangsu, China
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Аннотация

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.

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