The aim of this research is the preparation of a system based on mesoporous silica nanoparticles (MSN) for delivery of Rivastigmine hydrogen tartrate and investigating of the system cytotoxicity, with or without drugs, on the human brain neuroblastoma cells (SY5Y). Rivastigmine is a hydrophilic and a hydrophobic drug which is used for treatment of Alzimerʾs disease. In this study MSN were synthesized and characterized by scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectroscopy, x-ray diffraction, N2 adsorption isotherms, and z-potential analysis. Results showed that all MSN were spherical with the same structure. The mean size of nanoparticles was 100±13 nm and the mean diameter of pores was 2.15 nm. The loading capacity and efficiency of rivastigmine hydrogen tartrate were obtained 20.88, and 25%, respectively. Release of rivastigmine from nanoparticles in the simulated gastric and body fluid during 24 h were obtained 70.5 and 79.6%, respectively, which was shown the slightly fast release of rivastigmine in simulated gastric fluid. The cytotoxicity effect of nanoparticles with and without rivastigmine was done by MTT assay on SY5Y cell lines. Results showed that the in vitro rivastigmine release from the nanoparticles containing of it exhibited the more treatment property as free rivastigmine on SY5Y.