Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
Department of Pharmacy, 210th Hospital of People's Liberation Army, Dalian, Liaoning 116011, China.
J Nanosci Nanotechnol. 2020 Mar 1;20(3):1321-1331. doi: 10.1166/jnn.2020.16955.
In this study, a novel transferrin modified liposomal dioscin was prepared by the film dispersion method. The transferrin modified dioscin loaded liposomes (Tf-Lip/Dio) were near-spherical in morphology and had an average particle size of 140.07±1.33 nm, a narrow polydispersity index of <0.2 and a relatively stable zeta potential of -23.7±1.16 mV. The drug entrapment efficiency (EE) and drug loading (DL) of Tf-Lip/Dio were 88.94±1.02% and 4.16±0.05%, respectively. Tf-Lip/Dio exhibited a sustained release characterization of approximately 30% of the total dioscin content after 72 h at 37 °C. Tf-Lip/Dio showed higher cytotoxic efficacy after incubation for 24 h in both HeLa cells and HepG2 cells than in nonmodified liposomes. The enhanced antitumor activity of Tf-Lip/Dio might be due to the increased intracellular uptake, which was corroborated by laser scanning confocal microscopy and flow cytometry. Furthermore, hemolysis experiments preliminarily verified the safety of its intravenous injection. Overall, this study demonstrates Tf-Lip/Dio to be a favorable delivery vehicle for dioscin in future cancer therapy.
在这项研究中，通过薄膜分散法制备了一种新型转铁蛋白修饰的薯蓣皂苷脂质体。转铁蛋白修饰的薯蓣皂苷负载脂质体（Tf-Lip/Dio）呈近球形形态，平均粒径为 140.07±1.33nm，多分散指数<0.2，相对稳定的 Zeta 电位为-23.7±1.16mV。Tf-Lip/Dio 的药物包封效率（EE）和药物载量（DL）分别为 88.94±1.02%和 4.16±0.05%。Tf-Lip/Dio 在 37°C 下孵育 72 小时后，大约有 30%的薯蓣皂苷总含量呈现持续释放特征。Tf-Lip/Dio 在 HeLa 细胞和 HepG2 细胞中孵育 24 小时后，其细胞毒性作用均高于未修饰的脂质体。Tf-Lip/Dio 的抗肿瘤活性增强可能是由于细胞内摄取增加所致，这一点通过激光扫描共聚焦显微镜和流式细胞术得到了证实。此外，溶血实验初步验证了其静脉注射的安全性。总的来说，这项研究表明 Tf-Lip/Dio 是未来癌症治疗中薯蓣皂苷的一种有前途的递送载体。
