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Various stimuli-responsive gatekeepers, which endow the MSNs with on-demand drug delivery, surface modification strategies for targeting purposes, and multifunctional MSNs utilized in drug delivery systems (DDSs) are also addressed. Also, the capability of MSNs as flexible imaging platforms is considered. In addition, physicochemical attributes of MSNs and their effects on cancer therapy with a particular focus on recent studies is emphasized. Moreover, major challenges to the use of MSNs for cancer therapy, biosafety and cytotoxicity a