The cargoes loaded mesoporous silica nanoparticles (MSNs) and their versatile functions can facilitate releasing the drug at controlled manner, increase cellular uptake efficiency, targeting tumor zone with enhanced therapeutic efficacy against cancer. Herein, we designed dual drug loaded MSN nanocomposite for improving drug delivery. This investigation proves that the pore tunnels of mesoporous silica nanoparticles (MSN) were encapsulated with doxorubicin (DOX). The DOX loaded MSN was functional with polyethylene glycol (PEG)-cRGD peptide and Citraconic anhydride (CAH)-metformin (MT) at 1:3 ratio. The grafted PEG-cRGD improves MSN targeting abilty whereas the CAH supports the active release of the second drug MT at tumor microenvironment. Interstingly the polymer conjugated mesoporous silica (PMS) materials found to elevate the drug loading efficacy and effective facial uptake behaviors that support th enhanced cytotoxicity at both in vitro and in vivo levels. Thus, the outstanding quality of polymer conjugated mesoporous silica loaded with drugs exhibited excellent combined anti-tumor activity that atribute as a potential drug delivery podium for cancer therapy.