The combination of photothermal and chemotherapy execute by a single nanosystem is more effective in cancer therapy. The present study demonstrates that the chemo-photothermal therapy (chemo-PTT) using polydopamine (PDA) coated MoS2 nanoflowers (NFs) and subsequently, loaded with a subtherapeutic dose of gemcitabine (Gem), provide a robust anti-tumor effects. The folic acid (FA) is functionalized into the MoS2-PDA-Gem to improve the targeting functionality. It particularly recognizing the overexpressed folate receptor (FR) on tumor cell surfaces and it releases Gem into endocytic organelles of MDA-MB-231 cells upon FR-mediated endocytosis. The NFs were subsequently exposed to NIR (808 nm, 0.5 W cm(2), 5 min), it effectively induces the heat and it photothermal conversion efficiency (PCE) was calculated to be 33.6%. The hemolytic activity of MoS2 and MoS2-PDA-FA NFs was calculated to be 8 and 2.3% when incubated with sheep blood cells. The higher PCE of MoS2-gem-PDA-FA NFs enhanced ROS generation and 80% phototoxicity towards MDA-MB-231 cells. The FA conjugated NFs effectively target breast cancer cells and deliver the drug inside the cellular compartments. Cell death can be induced by combination therapy (PTT and drugs), which causes significant damage to the nucleus and mitochondria. Therefore, Using MoS2-PDA-gem-FA as an effective drug delivery platform and new avenues may open for developing cancer treatment strategies.