Facile synthesis of the lipid bilayer coated mesoporous silica nanocomposites and their application in drug delivery

• The lipid bilayer coated mesoporous silica nanocomposites (LMSNs) were successfully prepared.
• The LMSNs had improved dispersing stability and uptake efficiency compared with bare mesoporous silica nanoparticles (MSNs)
• The presence of the lipid bilayer could improve the biocompatibility and reliability of MSNs as drug carriers.
• The prepared LMSNs can load drug with high efficiency and improve the therapeutic efficacy of the encapsulated drugs.

The lipid bilayer coated mesoporous silica nanocomposites (LMSNs) were synthesized with aim to obtain better performance in the application of drug delivery. Phospholipids composed of soybean lecithin and DSPE-PEG 2000 were pre-prepared into liposomes, then they were allowed to fuse onto the mesoporous silica nanoparticles (MSNs) forming a surrounding lipid bilayer. The obtained LMSNs had an average particle size of 295 nm, zeta potential of −1.0 mV and a good dispersing stability in saline buffers. Facilitated by the affinity of the lipid bilayer with cell membrane, the internalization of LMSNs by cells was markedly increased. In addition, compared with bare MSNs, the cytotoxicity, hemolysis percentage and nonspecific BSA absorption of LMSNs were significantly reduced, making them become more reliable carriers for drug delivery. When encapsulating a model drug, doxorubicin (DOX) into LMSNs, the loading efficiency can reach as high as 16%. The obtained LMSNs-DOX exhibited a pH-responsive release behavior and the presence of the lipid bilayer did not significantly retard the release of DOX. Furthermore, LMSNs greatly enhanced the cellular accumulation and cytotoxicity of DOX toward the MCF-7 cells. In summary, the lipid bilayer coating was a simple and facile strategy to functionalize MSNs, and the obtained LMSNs exhibiting good biocompatibility were promising nanocarriers in improving the cellular uptake and therapeutic efficacy of anticancer drugs.

Figure optionsDownload as PowerPoint slide