Lipoamino acid-based cerasomes for doxorubicin delivery: Preparation and in vitro evaluation

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, zeta-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.