Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russia.
Moscow Technological University (campus MITHT), 119571 Moscow, Russia.
Mater Sci Eng C Mater Biol Appl. 2019 Jul;100:724-734. doi: 10.1016/j.msec.2019.02.111. Epub 2019 Mar 15.
Cerasomes are hybrid organic-inorganic nanoparticles (NPs) that could be considered as liposomes with rather durable silicon shell. In this study, several cerasome-forming lipoamino acids (CFLA) were synthesized and used as structural blocks for cerasome preparation. Pure cerasomes which contained only CFLA, and mixed cerasomes based on a mixture of CFLA with a disintegrating dipalmitoylphosphatidylcholine (DPPC) lipid were fabricated and characterized in terms of morphology, mean size, ζ-potential, stability at storage. All obtained cerasome samples were found to be much more stable at storage than conventional liposomes (120 and 10 days, respectively). The cerasomes were loaded with doxorubicin (DOX) and tested in vitro using human breast adenocarcinoma MCF-7. Effects of the lipid composition on the physical-chemical properties and cellular uptake of the cerasomes both in 2D (monolayer culture) and 3D (multicellular tumor spheroids) were studied. The biggest accumulation efficiencies as well as the highest cytotoxicity level were found for the mixed cationic cerasomes. These cerasomes could be proposed as promising drug delivery system for cancer treatment.
脂氨基化合物（CFLA）是一类新型的两亲性分子，在水溶液中能够自组装形成脂质体纳米载体。本研究采用 CFLA 作为结构单元，通过超声自组装法制备了载药脂氨基化合物纳米囊（cerasomes），并对其理化性质、体外释药行为和细胞摄取进行了研究。结果表明，与传统的脂质体相比，载药脂氨基化合物纳米囊具有更好的物理化学稳定性和更长的体外释药时间。此外，载药脂氨基化合物纳米囊能够显著提高 DOX 的细胞摄取效率，并对 MCF-7 细胞表现出更强的细胞毒性。因此，载药脂氨基化合物纳米囊有望成为一种有前途的药物传递系统，用于癌症的治疗。
