Lithium modified bioactive glass nanoparticles were prepared for multiple deliveries of lithium ions and drugs. The particle size, structure and thermal behavior of nanoparticles were analyzed using TEM, FTIR and DSC respectively. The porosity% and specific surface area of glass nanoparticles were about 68.6% and 224.92 (m2/g), respectively. The in vitro bioactivity evaluation in SBF revealed that glass nanoparticles were capable of inducing apatite layer over their surfaces. This could be considered as a good indicator for their future abilities to regenerate bone tissue in vivo. Also, lithium ions were released from glass nanoparticles via diffusion controlled process which could activate Wnt signaling pathway and enhance osteogenesis. As a final point, the possibility of utilizing the glass nanoparticles as a controlled delivery device for vancomycin or 5-FU was verified. Fitting vancomycin or 5-FU release profiles to various mathematical models pointed out that both drugs were released by a diffusion-controlled mode.