The purpose of this study is to prepare galactosyl modified
lipid bilayer-coated mesoporous
silica nanoparticles (GPEM) to enhance the antitumor efficacy against
hepatocellular carcinoma cells. The
irinotecan (CPT-11) loaded mesoporous
silica nanoparticles (MSNs) was coated with the Gal-P123 modified functional
lipid bilayer by thin-film dispersion method. Nanoparticles were characterized with particle size, zeta potential, morphology and drug release in vitro. Afterwards, the cell uptake, intracellular concentration of
CPT-11, cell apoptosis rate and cytotoxicity were evaluated on human
hepatocellular carcinoma cell line Huh-7. The results showed that MSNs were coated with intact
lipid bilayers and the nanoparticles had clear core-shell structure. GPEM is stable with the mean particle size of (78.01 +/- 2.04) nm. The low leakage rate in normal physiological conditions in vitro is contributed to the protection of stable
lipid bilayer, and the fast drug release in
acid environment due to the destruction of the
lipid bilayer. On the cell level, the vector could improve the intracellular
CPT-11 concentration by 4 times because of the functional
lipid bilayer. The high
CPT-11 concentration led to the increasement of apoptosis rate by 48.6%, and the reduction of half maximal inhibitory concentration (IC50) values of
CPT-11 by 2 times, indicating stronger cell cytotoxicity.