The invention relates to the technical field of medicines, and provides ruthenium complex loaded mesoporous silicon nanoparticles RuNPs. The ruthenium complex loaded mesoporous silicon nanoparticles consist of mesoporous silicon nanospheres MSNs, ruthenium complexes RuNHC which are loaded on the mesoporous silicon nanospheres MSNs, and biotinylated chitosan CTS-Biotin covering the ruthenium complex loaded mesoporous silicon nanospheres MSNs. The nanoparticles RuNPs provided by the invention, compared with RuNHC in the prior art, can achieve controlled release and targeted delivery on the RuNHC complex, and meanwhile, the nanoparticles RuNPs have a pH-responsive controlled-release performance; the nanoparticles RuNPs not only can improve an antineoplastic activity but also can enhance a targeting performance to tumor cells; and toxic and side effects on normal tissues and cells can be reduced.