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In the past decade, mesoporous silica nanoparticles (MSNs) have attracted increasing attention for their potential biomedical applications. With their tailored mesoporous structure and high surface area, MSNs as drug delivery systems (DDSs) show significant advantages over traditional drug nanocarriers. MSNs have the characteristics of large specific surface area and large pore volume, easy to be modified on the inner and outer surfaces, high drug loading and high targeting ability, thus showing a wide application prospect. In this paper, the influencing factors, functionalization of MSNs synthesis method and drug delivery system were introduced, and the environmental response in drug releasing were also reviewed.