The targeted delivery of therapeutics to the kidneys has a profound potential for the management of renal fibrosis. Thus, we developed a drug delivery system that targets mesangial cells by conjugating anti-alpha8 integrin to the surface of liposomes. We coloaded emodin (EMO) and diammonium glycyrrhizinate (DAG) to the immunoliposomes for combined therapy. The coloaded immunoliposomes were small size (), narrowly distributed, and with nearly neutral zeta potential and good stability. The encapsulation rate of EMO and DAG in immunoliposomes was and , respectively. Using a BCA assay, the actual number of antibody molecules attached to a single liposome was determined as being approximately 41. An in vitro release study showed that EMO and DAG could be ratiometrically released from the immunoliposomes, which means that an optimized synergistic ratio of the two drugs could be achieved. Studies on cellular uptake studies demonstrated an approximately 3-fold increase for immunoliposomes in HBZY-1 cells compared to nonconjugated liposomes. In vitro cell growth inhibition and Western Blot assay revealed that the coloaded immunoliposomes exhibited a stronger and synergistic in vitro antifibrosis effect against NIH3T3 and HBZY-1 cells in vitro. Taken together, it indicated that anti-alpha8 integrin-modified immunoliposomes for codelivery of EMO and DAG have great potential for targeting the kidneys for the treatment of renal fibrosis.

中文翻译：

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大黄素和甘草酸二铵通过抗α8整合素结合的免疫脂质体的代码传递治疗肾纤维化。

向肾脏的靶向治疗药物在控制肾纤维化方面具有深远的潜力。因此，我们开发了一种通过将抗α8整联蛋白缀合到脂质体表面来靶向肾小球系膜细胞的药物递送系统。我们将大黄素（EMO）和甘草酸二铵（DAG）负载到免疫脂质体上进行联合治疗。负载的免疫脂质体体积小（），分布狭窄，并且具有接近中性的Zeta电位和良好的稳定性。免疫脂质体中EMO和DAG的包封率为 和 ，分别。使用BCA分析，确定与单个脂质体连接的抗体分子的实际数量约为41。体外释放研究表明，EMO和DAG可以按比例从免疫脂质体中释放出来，这意味着优化的脂质体协同比例可以达到两种药物。细胞摄取研究表明，与非缀合脂质体相比，HBZY-1细胞中免疫脂质体增加了约3倍。体外细胞生长抑制和蛋白质印迹分析，得知coloaded免疫脂质体表现出比和协同的体外对NIH3T3和HBZY-1细胞抗纤维化作用的体外。两者合计，表明抗α8整联蛋白修饰的免疫脂质体可用于EMO和DAG的代码传递，具有靶向肾脏以治疗肾纤维化的巨大潜力。