Abstract

Silymarin (SM) from Silybum marianum (L.) is a sum of flavolignans (silibinin, silychristin, silydianin, and isosilibinin), exhibiting a wide spectrum of biological activity and having anti-inflammatory, antitumor, hepatoprotective, immunomodulatory effects. Using a modified emulsion method with solvent evaporation, lipid nanoparticles with silymarin (LNP-SM) were obtained, the size of which was 257 ± 6 nm, and the ζ potential was –20.8 ± 1.6 mV. The efficiency of SM inclusion in the LNP-SM was 89.8%, the loading degree was 5.4%. The release of CM from the composition of the resulting nanoparticles was prolonged; after 48 h, only 68.3 ± 5.4% of the active substance was released into the dialysis medium. The dynamics of the inclusion/release of SM in the composition of LNP into the films of bacterial cellulose (BC) produced by the Gluconacetobacter hansenii GH-1/2008 strain has been studied. It was shown, that after 24 h of incubation the maximum of BC film saturation with SM reached 0.745 ± 0.038 mg/cm², and the maximum release was 0.520 ± 0.041 mg/cm². It was demonstrated that both LNP-SM sols and samples of BC saturated with LNP-SM exhibited low hemolytic activity, which indicates the potential biosafety of these preparations. The preparation LNP-SM, in contrast to free SM, exhibited fungistatic action against the fungi of A. niger and C. albicans. Both free SM and LNP-SM suppressed the growth of gram-positive bacteria; however, the effect of LNP-SM was much more effective. The minimum inhibitory concentration of the LNP-SM preparation for B. subtilis and B. coagulans was 105 and 210 μg/mL, respectively. The possibility of developing biocompatible coating materials based on BC saturated with LNP-SM is discussed.

中文翻译：

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脂质纳米颗粒组合物中含有水飞蓟素黄酮素的细菌纤维素的饱和度

摘要

来自水飞蓟的水飞蓟素 (SM)(L.) 是黄酮素（水飞蓟素、水飞蓟素、水飞蓟素和异水飞蓟素）的总和，具有广泛的生物活性，并具有抗炎、抗肿瘤、保肝、免疫调节作用。使用改进的溶剂蒸发乳化法，获得了含有水飞蓟素的脂质纳米粒（LNP-SM），其尺寸为 257 ± 6 nm，ζ 电位为 –20.8 ± 1.6 mV。LNP-SM中SM夹杂效率为89.8%，负载度为5.4%。CM从所得纳米颗粒的组合物中的释放被延长；48 小时后，只有 68.3 ± 5.4% 的活性物质释放到透析介质中。LNP组合物中SM的包含/释放动力学进入由汉森葡糖酸杆菌产生的细菌纤维素（BC）膜中已经研究了 GH-1/2008 菌株。结果表明，培养24小时后，BC膜与SM的最大饱和度达到0.745±0.038mg/cm ²，最大释放为0.520±0.041mg/cm ²。结果表明，LNP-SM 溶胶和用 LNP-SM 饱和的 BC 样品均表现出低溶血活性，这表明这些制剂具有潜在的生物安全性。与游离 SM 相比，LNP-SM 制剂对黑曲霉和白色念珠菌的真菌具有抑菌作用。游离 SM 和 LNP-SM 均抑制革兰氏阳性菌的生长；然而，LNP-SM 的效果要好得多。LNP-SM 制剂对枯草芽孢杆菌和凝结芽孢杆菌分别为 105 和 210 μg/mL。讨论了开发基于用 LNP-SM 饱和的 BC 的生物相容性涂层材料的可能性。