Solid Dispersions of Genistein via Solvent Rotary Evaporation for Improving Solubility, Bioavailability, and Amelioration Effect in HFD-Induced Obesity Mice

染料木素 生物利用度 溶解度 溶剂 蒸发 化学 减肥 肥胖 化学工程 药理学 色谱法 材料科学 内科学 医学 有机化学 热力学 工程类 物理
作者
Chenxu Qiu,Yancui Zhang,Yingsai Fan,Shupeng Li,Jianting Gao,Xin He,Xinghua Zhao
出处
期刊:Pharmaceutics [Multidisciplinary Digital Publishing Institute]
卷期号:16 (3): 306-306 被引量:3
标识
DOI:10.3390/pharmaceutics16030306
摘要

Genistein (GEN) is an active pharmaceutical ingredient that presents the challenges of poor water solubility and low oral bioavailability. To tackle these challenges, a GEN solid dispersion was prepared by solvent rotary evaporation using polyvinylpyrrolidone K30 (PVP K30) as a carrier. The optimal formulation was determined by drug loading efficiency and in vitro release. The physical state of the solid dispersion was characterized by DSC, XRD, SEM and FT-IR. And the results of the in vitro release study indicate that the drug release of SD (1:7) increased 482-fold that of pure GEN at 60 min. Following oral administration to rats, the Cmax and AUC0–24 of SD (1:7) was increased 6.86- and 2.06-fold to that of pure GEN. The adipose fat index and body weight of the SD (1:7) group were significantly lower than those of the GEN group (p < 0.05). Meanwhile, the levels of TC and TG in the serum were significantly decreased in the SD (1:7) group compared with the GEN group (p < 0.05). All experiments revealed that solid dispersion could be a promising formulation approach to improve the dissolution rate, oral bioavailability, and effect on the reduction of lipid accumulation in high-fat diet-induced obesity mice.
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