An efficient enzyme-responsive controlled release carrier system was successfully fabricated using single-stranded DNA encapsulated functional mesoporous silica nanoparticles. Mesoporous silica nanoparticles were initially fabricated through hydrolysis of tetraethyl orthosilicate (TEOS) in cetyltrimethylammonium chloride (CTAC) solution, and the surface of nanoparticles could be encapsulated with single-stranded DNA. This nanomaterial has excellent bioactivity and its hydrolysate cannot cause damage to normal cell, thus the biocompatibility of the nanomaterial is improved. In addition, this nanomaterial showed an excellent drug release performance when loaded with drugs, which would be helpful to increase the treatment efficiency and decrease side effects of drugs.