Recent advances in novel drug delivery system aims to enhance the safety and efficacy of drug molecule by formulating a convenient dosage form for ease of administration and to achieve better patient compliance. A number of approaches are available in delivering therapeutic substance to the target site in sustained and controlled release fashion. Recent development in drug delivery system uses a variety of carriers has resulted in a revolutionary approach towards diagnosis and therapy. Mesoporous silica nanoparticles have been a potent nanocarriers for many different therapeutic agents, i.e., the surface functionalization of silica nanoparticles with chemical agents, polymers, and supramolecular moieties enable the efficient delivery of therapeutic agents in a highly controlled system. Also, materials needed with high thermal, chemical, mechanical properties, toxicity, biosafety, and in vivo efficiency involving biodistribution, pharmacokinetics, biodegradation, and excretion of MSNs. Development of MSNs as carriers for target drug delivery systems has increased exponentially during the last few days. The present work is focused on the mechanisms, synthesis, characteristics and application of mesoporous silica nanoparticles. In this review, we summarize the facts about mesoporous silica nanoparticles drug delivery systems comprehensively. This review also provides the detailed concept of mesoporous silica nanoparticles a novel approach for drug targeting.