The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H₂O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

中文翻译：

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改进的乳液蒸发法制备PEG-PLA染料木黄酮胶束

这项研究的目的是通过用聚乙二醇-聚乳酸（PEG-PLA）共聚物包封来提高染料木黄酮的生物利用度。使用改良的乳液蒸发法制备的染料木素胶束（GMs）比原始方法制备的胶束更稳定。聚乙烯醇，吐温80，超声处理时间，PEG-PLA /染料木黄酮比率和有机相（丙酮）/ H _2的影响研究了O比对GM的大小，多分散指数，包封率和载药率的影响。获得了GM，并在最佳实验条件下对其进行了表征。为了长期保存，通过用海藻糖冷冻干燥将GMs冻干以产生染料木黄酮冻干粉（GLP）。用傅里叶变换红外光谱和差示扫描量热法分析GLP表明，染料木黄酮已成功地掺入胶束结构中。体外释放实验表明，将染料木黄酮掺入PEG-PLA共聚物中可显着提高其溶解度和生物利用度。与金雀异黄素相比，GLP在抑制HSC-T6细胞增殖方面更有效。治疗GLP 10-20  μ克/ mL的48小时显著抑制的蛋白质表达α肌动蛋白平滑肌肌和I型胶原蛋白在HSC-T6细胞与对照组相比。这些数据表明，染料木素以GLP的形式改善了溶解度和生物利用度，增强了其在体外的抗纤维化作用。