A　targeting　drug　delivery　system　(TDDS)　can　selectively　deliver　antitumor　drugs　to　cancerous　parts　to　improve　its　anticancer　efficacy.　Hence,　a　targeted　drug　delivery　system　(UA/siVEGF@MSN-FA)　coloading　ursolic　acid　(UA)　and　vascular　endothelial　growth　factor　(VEGF)　targeted　siRNA　(siVEGF)　based　on　mesoporous　silica　(MSN)　nanocarrier　modified　by　a　folic　acid　(FA)　molecule　was　designed　and　synthesized.　The　MSN-FA　nanoparticles　were　investigated　for　shape,　diameter,　and　zeta　potential　and　and　by　infrared　(IR)　spectroscopy.　FR-overexpressing　HeLa　cells　and　FR-negative　HepG2　cell　lines　were　used　to　evaluate　the　in　vitro　cellular　uptake　and　the　cytotoxicity　of　MSN-FA　nanoparticles.　The　morphology　of　HeLa　cells　transfected　with　siVEGF@MSN-FA　was　observed　using　fluorescence　microscopy.　Our　findings　demonstrated　that　UA@MSN-FA　nanoparticles　were　near-spherical,　and　the　particle　size　was　about　209　±　9.21　nm.　The　MSN-FA　nanocarrier　not　only　could　enhance　the　in　vitro　transfection　efficiency　and　the　stability　of　siVEGF　but　also　could　further　improve　the　targeted　anticancer　efficacy　of　UA　and　siVEGF　via　the　active　targeting　property　of　FA.　Overall,　the　MSN-FA　drug　delivery　system　could　serve　as　an　excellent　material　in　biomedical　applications.　©　2017　American　Chemical　Society.