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Despite insolubility, non-specificity and high toxicity of therapeutics associated with biological obstacles such as drug resistance, blood-brain barrier and systemic enzymatic degradation, patients have to take their high dosages to attain the expected therapeutic efficacy for the disease-treatment. To overcome these complications, various drug carriers are being investigated in the pharmaceuticals to supply their therapeutics to the specific sites in the body. Nowadays, mesoporous silica nanoparticles (MSNPs) have emerged as promising candidate because they can overcome all the barriers maximally by producing their biological effectiveness in a controlled and sustained manner to the diseased site. As the mesoporous silica materials have the excellent favorable physicochemical features, the multi-functionalized MSNPs are capable to target and release their cargos into the diseased cells according to the requirement upon exposition to external or internal stimuli. This review demonstrates the state of knowledge for the consideration MSNPs as delivery system against various diseases.