Pterostilbene has shown very promising traits as a nutraceutical compound, especially in the field of cancer treatment. However, its poor aqueous solubility hinders its clinical applicability. The purpose of this work was to enhance the antitumoral activity of pterostilbene in hepatic cancer via encapsulation in lipid nanocapsules. Pterostilbene nanocapsules were prepared using the phase inversion technique. One gram of Kolliphor® HS 15 dissolved in 3 g of distilled water was added to 1 g of isopropyl myristate containing 150 mg Epikuron 200 and 100 mg pterostilbene under magnetic stirring, while applying three temperature cycles alternating between 55 and 85 °C for phase inversion to occur. Shock cooling of the dispersion was induced by introduction of 5 g of distilled water, followed by stirring for 30 min. The nanocapsules were characterized for the particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading, morphology, antitumoral activity in HepG2 liver cancer cell line in terms of viability, assessment of cell death mode and cycle arrest, cellular localization assessment, and quantification of cellular uptake. The in vivo antitumoral activity of lipid nanocapsules was further verified using a chemically-induced hepatic cancer model using diethylnitrosamine and carbon tetrachloride. Several biochemical markers were quantified, followed by histopathological examination. Results displayed the potential of pterostilbene in treatment of liver cancer, with the enhancement of its therapeutic efficacy by encapsulation in lipid nanocapsules, as evidenced by further decreased levels of ALT, AST, AFP, Bcl2, VEGF, NF-kB, ERK, AKT, with concomitant increase in caspase3 level, while showing comparable histological features to the normal control group. Pterostilbene nanocapsules were proven promising in the treatment of hepatocellular carcinoma, deserving further preclinical and clinical evaluation.

作为一种营养保健化合物，紫檀芪已显示出非常有前途的特性，特别是在癌症治疗领域。但其水溶性差限制了其临床应用。这项工作的目的是通过脂质纳米胶囊的封装来增强紫檀芪在肝癌中的抗肿瘤活性。采用相转化技术制备了紫檀芪纳米胶囊。将 1 克 Kolliphor® HS 15 溶解在 3 g 蒸馏水中，在磁力搅拌下添加到 1 g 含有 150 mg Epikuron 200 和 100 mg 紫檀芪的肉豆蔻酸异丙酯中，同时应用 55 至 85 °C 之间交替的三个温度循环进行相转化发生。通过引入5g蒸馏水引发分散体的骤冷，然后搅拌30分钟。对纳米胶囊的粒径、多分散指数、zeta 电位、包封效率、载药量、形态、HepG2 肝癌细胞系的抗肿瘤活性（活力、细胞死亡模式和周期停滞评估、细胞定位评估）进行了表征。细胞摄取的量化。使用二乙基亚硝胺和四氯化碳化学诱导的肝癌模型进一步验证了脂质纳米胶囊的体内抗肿瘤活性。对几种生化标记物进行定量，然后进行组织病理学检查。结果显示紫檀芪在治疗肝癌方面具有潜力，通过脂质纳米胶囊封装可增强其治疗效果，进一步降低ALT 、 AST 、 AFP 、 Bcl2 、 VEGF 、 NF-kB 、 ERK 、 AKT 水平。伴随着 caspase3 水平的增加，同时显示出与正常对照组相当的组织学特征。紫檀芪纳米胶囊在治疗肝细胞癌方面被证明具有广阔的前景，值得进一步的临床前和临床评价。