肝细胞癌（HCC）是一种恶性肿瘤，影响许多被诊断患有肝细胞炎症和肝硬化的患者。靶向聚合物纳米胶囊可以促进抗癌药物的内化和积累。制备了双靶向叶酸/乳糖酸-聚乳酸共乙醇酸纳米胶囊（NC），并负载紫檀芪（PTN），并表征了其理化性质以及体外和体内抗癌活性。 NCs 的尺寸为 222 nm，zeta 电位为 - 16.5 mV，缓释时间为 48 小时。流式细胞术显示，PTN NCs (5.87±0.8 µg/mL) 对 HepG2 肝癌细胞的 IC50 (5.87±±0.8 µg/mL) 比未封装的 PTN (121.26±9.42 µg/mL) 低 20 倍，因为前者的细胞摄取增强。对 HCC 诱导动物的体内研究表明，双靶向 NC 相对于未封装的 PTN 具有优越性，它显着降低了肝脏标志物 ALT、AST 和 ALP，以及肿瘤相关标志物 AFP 和 Bcl2，并提高了抗凋亡标志物 caspase 3。此外，NCs 显着降低了氧化应激，并表现出与正常组几乎相当的组织学特征。因此，可以得出结论，双连接叶酸/乳糖酸纳米胶囊可被认为是肝细胞癌的一种有前途的潜在治疗选择。© 2023。控释协会。

Hepatocellular carcinoma (HCC) is a malignant tumor that affects many patients diagnosed with hepatic cell inflammation and liver cirrhosis. Targeted polymeric nanocapsules could facilitate the internalization and accumulation of anticancer drugs. Dual-targeted folic acid/lactobionic acid-poly lactic co-glycolic acid nanocapsules (NCs) were prepared and loaded with pterostilbene (PTN) and characterized for their physicochemical properties, as well as in vitro and in vivo anticancer activity. NCs displayed a size of 222 nm, zeta potential of - 16.5 mV, and sustained release for 48 h. The IC50 of PTN NCs (5.87 ± 0.8 µg/mL) was 20 times lower than unencapsulated PTN (121.26 ± 9.42 µg/mL) on HepG2 liver cancer cells owing to the enhanced cellular uptake of the former, as delineated by flow cytometry. In vivo study on HCC-induced animals delineated the superiority of the dual-targeted NCs over the unencapsulated PTN, which significantly reduced the liver markers ALT, AST, and ALP, as well as the tumor-related markers AFP and Bcl2, and elevated the anti-apoptotic marker caspase 3. Furthermore, the NCs significantly reduced the oxidative stress and exhibited almost comparable histological features to the normal group. Therefore, it can be concluded that the dual-ligated folic acid/lactobionic acid nanocapsules can be considered a promising potential treatment option for hepatocellular carcinoma.© 2023. Controlled Release Society.