This study aimed to increase the solubility of glycyrrhetinic acid (GA) in water and enhance its liver-targeting ability using self-assembling nanomicelles (NMs) based on stearic acid-modified fenugreek gum (FG-C18). The GA/FG-C18 NMs were prepared by an ultrasonication dispersion method. The nanomicelles were spherical particles with a particle size of 198.61 ± 1.58 nm and a zeta potential of -30.12 ± 0.28 mV. The drug loading and encapsulation efficiency were 13.34 ± 0.24% and 80.07 ± 1.44%, respectively. The results of differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) indicated that GA was successfully encapsulated into the nanomicelles in a molecularly dispersed state. An in vitro release test showed that GA/FG-C18 NMs possessed a slow drug release profile in PBS (pH 7.4) over 200 h. The cytotoxicity assay indicated that GA/FG-C18 NMs showed much higher inhibitory efficacy in HepG2 cells than in MCF-7 cells. Tissue section studies indicated that the accumulation of DiR-loaded FG-C18 nanomicelles in the liver of mice was higher than that of the DiR solution, and the fluorescence intensity decreased over time. GA/FG-C18 NMs showed a larger area under the curve (AUC) and mean residence time (MRT) compared with free GA after intravenous administration in mice. The in vivo studies showed that GA mainly accumulated in the liver after encapsulation by FG-C18 NMs, and the drug concentration was higher than that of free GA. These results suggested that FG-C18 NMs could serve as a potential drug delivery system for targeting GA to liver tissue.

中文翻译：

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通过基于硬脂酸修饰的胡芦巴胶的纳米胶束对甘草次酸进行肝靶向。

这项研究旨在使用基于硬脂酸修饰的胡芦巴胶（FG-C18）的自组装纳米胶束（NMs）来增加甘草次酸（GA）在水中的溶解度并增强其肝靶向能力。通过超声分散法制备GA / FG-C18 NM。纳米胶束是球形颗粒，粒径为198.61±1.58 nm，ζ电势为-30.12±0.28 mV。载药量和包封效率分别为13.34±0.24％和80.07±1.44％。差示扫描量热法（DSC）和X射线粉末衍射法（XRD）的结果表明，GA以分子分散状态成功地被包封到纳米胶束中。体外释放试验表明，GA / FG-C18 NMs在PBS（pH 7.4）中在200小时内具有缓慢的药物释放特性。细胞毒性试验表明，GA / FG-C18 NMs对HepG2细胞的抑制作用远高于MCF-7细胞。组织切片研究表明，负载DiR的FG-C18纳米胶束在小鼠肝脏中的积累高于DiR溶液，并且荧光强度随时间降低。与在小鼠中静脉内给药后的游离GA相比，GA / FG-C18 NMs的曲线下面积（AUC）和平均停留时间（MRT）更大。体内研究表明，GA被FG-C18 NMs包封后主要聚集在肝脏中，药物浓度高于游离GA。这些结果表明，FG-C18 NMs可以作为潜在的将GA靶向肝组织的药物递送系统。组织切片研究表明，负载DiR的FG-C18纳米胶束在小鼠肝脏中的积累高于DiR溶液，并且荧光强度随时间降低。与在小鼠中静脉内给药后的游离GA相比，GA / FG-C18 NMs的曲线下面积（AUC）和平均停留时间（MRT）更大。体内研究表明，GA被FG-C18 NMs包封后主要聚集在肝脏中，药物浓度高于游离GA。这些结果表明，FG-C18 NMs可以作为潜在的将GA靶向肝组织的药物递送系统。组织切片研究表明，负载DiR的FG-C18纳米胶束在小鼠肝脏中的积累高于DiR溶液，并且荧光强度随时间降低。与在小鼠中静脉内给药后的游离GA相比，GA / FG-C18 NMs的曲线下面积（AUC）和平均停留时间（MRT）更大。体内研究表明，GA被FG-C18 NMs包封后主要聚集在肝脏中，药物浓度高于游离GA。这些结果表明，FG-C18 NMs可以作为潜在的将GA靶向肝组织的药物递送系统。与在小鼠中静脉内给药后的游离GA相比，GA / FG-C18 NMs的曲线下面积（AUC）和平均停留时间（MRT）更大。体内研究表明，GA被FG-C18 NMs包裹后主要聚集在肝脏中，药物浓度高于游离GA。这些结果表明，FG-C18 NMs可以作为潜在的将GA靶向肝组织的药物递送系统。与在小鼠中静脉内给药后的游离GA相比，GA / FG-C18 NMs的曲线下面积（AUC）和平均停留时间（MRT）更大。体内研究表明，GA被FG-C18 NMs包封后主要聚集在肝脏中，药物浓度高于游离GA。这些结果表明，FG-C18 NMs可以作为潜在的将GA靶向肝组织的药物递送系统。