a Department of Radiation Oncology , Ruijin Hospital, Shanghai Jiaotong University School of Medicine , Shanghai , China.
b Department of Oncology , Ruijin Hospital, Shanghai Jiaotong University School of Medicine , Shanghai , China.
Artif Cells Nanomed Biotechnol. 2018 Dec;46(8):1902-1907. doi: 10.1080/21691401.2017.1396222. Epub 2017 Oct 28.
The aim of this study to develop galactosylated erlotinib liposomes for treatment of lung cancer. The liposomes were prepared by using solvent evaporation method. Various parameters such as particle size, zeta potential, entrapment efficiency, stability and in vitro drug release were determined. The size of liposomes (both conventional and modified) was 103.5 and 121.4 nm. The zeta potential and EE of both liposomes were -7.1 ± 1.3 mV, -1.2 ± 0.5 mV and (82.3 ± 1.9)%, (83.4 ± 1.5)%, respectively. It was found that modified liposomes increase the size of particles. The in vitro release results indicated that the release of erlotinib from galactosylated liposomes was similar to that of conventional liposome, demonstrating that the modification did not affect erlotinib release. From the result of in vivo, it proved that erlotinib liposomes can significantly improve the drug targeting, rapidly distribute the drug in the body, prolong the drug circulation time and significantly increase the relative bioavailability of the drug. Biodistribution studies showed that erlotinib from galactosylated liposomes had higher AUC inside liver than the injection group and no histological change occurred to the rat liver after the administration of erlotinib conventional and galactosylated liposomes.
本研究旨在开发半乳糖化厄洛替尼脂质体用于治疗肺癌。脂质体采用溶剂蒸发法制备。测定了各种参数，如粒径、Zeta 电位、包封效率、稳定性和体外药物释放。脂质体（常规和修饰）的粒径为 103.5nm 和 121.4nm。两种脂质体的 Zeta 电位和 EE 分别为-7.1±1.3mV、-1.2±0.5mV 和（82.3±1.9）%、（83.4±1.5）%。结果表明，修饰后的脂质体增加了颗粒的粒径。体外释放结果表明，半乳糖化脂质体中厄洛替尼的释放与常规脂质体相似，表明修饰不影响厄洛替尼的释放。体内结果证明，厄洛替尼脂质体能显著提高药物靶向性，使药物在体内迅速分布，延长药物循环时间，显著提高药物的相对生物利用度。分布研究表明，半乳糖化脂质体中的厄洛替尼在肝脏中的 AUC 高于注射组，并且在给予厄洛替尼常规和半乳糖化脂质体后，大鼠肝脏未发生组织学变化。
