Ming Yue, Li Bin, Fu Ruoqiu, Xing Haiyan, Liu Yao, Duan Dongyu, Li Ziwei, Li Li, Ni Rui, Xu Jing, Li Chen, Xiang Mingfeng, Song Hongyu, Chen Jianhong
Department of Pharmacy, Daping Hospital, Army Medical University, Chongqing, 400042, P. R. China.
J Nanosci Nanotechnol. 2021 Oct 1;21(10):5075-5082. doi: 10.1166/jnn.2021.19362.
Hepatocellular carcinoma (HCC) is the most common primary malignancy of the liver. The majority of patients with HCC are diagnosed with advanced-stage disease. Sorafenib is a frontline therapy drug approved by the Food and Drug Administration for advanced HCC. However, the poor aqueous solubility of sorafenib limits its applications. The present study aimed to overcome this limitation of sorafenib. Thus, bovine serum albumin (BSA)-based nanoparticles were developed to encapsulate hydrophobic sorafenib. The resultant sorafenib-loaded BSA nanoparticles (Sf-BSA-NPs) were thoroughly characterized for size distribution, encapsulation efficiency and morphology. Previous studies on HepG2 cells have demonstrated that Sf-BSA-NPs exhibit remarkable superiority to free sorafenib in cytocompatibility, cytotoxicity and proapoptotic effect. The results of the present study demonstrated that Sf-BSA-NPs were effective in improving aqueous solubility, and enhanced drug cytotoxicity, suggesting its therapeutic potential for HCC.
肝细胞癌(HCC)是最常见的肝脏原发性恶性肿瘤。大多数HCC患者被诊断为晚期疾病。索拉非尼是美国食品药品监督管理局批准用于晚期HCC的一线治疗药物。然而,索拉非尼较差的水溶性限制了其应用。本研究旨在克服索拉非尼的这一局限性。因此,开发了基于牛血清白蛋白(BSA)的纳米颗粒来包裹疏水性的索拉非尼。对所得的载索拉非尼牛血清白蛋白纳米颗粒(Sf-BSA-NPs)的尺寸分布、包封率和形态进行了全面表征。先前对HepG2细胞的研究表明,Sf-BSA-NPs在细胞相容性、细胞毒性和促凋亡作用方面比游离索拉非尼具有显著优势。本研究结果表明,Sf-BSA-NPs在提高水溶性方面有效,并增强了药物细胞毒性,表明其对HCC的治疗潜力。