Abstract Hepatocellular carcinoma (HCC) is one of the most common causes of cancer-related mortality worldwide. Sorafenib acts as a potential anticancer agent, but it shows less aqueous solubility, so its clinical application is limited. In this present study, we developed Sora-surface decorated iRGD (small cyclic peptide motif (CRGDK/RGPD/EC)) nanoparticles (labelled Sora-NPs and iRGD@Sora-NPs, respectively) to enhance its aqueous formulation and improve the anticancer activity of Sora. The synthesized Sora-NPs and iRGD@Sora-NPs confirmed by various spectroscopies and electroscopic techniques. Sora-NPs and iRGD@Sora-NPs dramatically suppressed the proliferation of hepatocellular carcinoma cells (BEL-7402 and Huh-7) and showed low toxicity in MTT assays. Compared with free Sora and Sora-NPs, iRGD@Sora-NPs significantly induces the apoptosis in hepatocellular carcinoma cells. The morphological changes were evaluated via various biochemical staining techniques (AO-EB and nuclear staining). Further, the apoptosis mode of hepatocellular carcinoma cell death was confirmed via flow cytometry analysis. Furthermore, the Sora-NPs and iRGD@Sora-NPs promoted apoptotic manner of cell death by G2/M phase arrest. In this present study explained that iRGD@Sora-NPs as a safe and hopeful strategy for chemotherapeutics of hepatocellular carcinoma therapy and deserve further clinical evaluations.

中文翻译：

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9-氨基酸环肽修饰的索拉非尼聚合物纳米粒用于肝细胞癌的高效体外护理分析

摘要 肝细胞癌 (HCC) 是全球癌症相关死亡的最常见原因之一。索拉非尼作为一种潜在的抗癌剂，但其水溶性较差，因此其临床应用受到限制。在本研究中，我们开发了 Sora 表面装饰的 iRGD（小环肽基序（CRGDK/RGPD/EC））纳米粒子（分别标记为 Sora-NPs 和 iRGD@Sora-NPs）以增强其水性配方并提高抗癌活性索拉。合成的 Sora-NPs 和 iRGD@Sora-NPs 通过各种光谱和电镜技术证实。Sora-NPs 和 iRGD@Sora-NPs 显着抑制肝细胞癌细胞（BEL-7402 和 Huh-7）的增殖，并在 MTT 测定中显示出低毒性。与免费的 Sora 和 Sora-NPs 相比，iRGD@Sora-NPs 显着诱导肝细胞癌细胞凋亡。通过各种生化染色技术（AO-EB 和核染色）评估形态变化。此外，通过流式细胞术分析证实了肝细胞癌细胞死亡的凋亡模式。此外，Sora-NPs 和 iRGD@Sora-NPs 通过 G2/M 期阻滞促进细胞死亡的凋亡方式。在本研究中，iRGD@Sora-NPs 作为肝细胞癌化疗的一种安全且有希望的策略，值得进一步的临床评估。此外，Sora-NPs 和 iRGD@Sora-NPs 通过 G2/M 期阻滞促进细胞死亡的凋亡方式。在本研究中，iRGD@Sora-NPs 作为肝细胞癌化疗的一种安全且有希望的策略，值得进一步的临床评估。此外，Sora-NPs 和 iRGD@Sora-NPs 通过 G2/M 期阻滞促进细胞死亡的凋亡方式。在本研究中，iRGD@Sora-NPs 作为肝细胞癌化疗的一种安全且有希望的策略，值得进一步的临床评估。