This research work involves multifunctional magnetically targeted drug delivery microspheres for treatment against breast cancer. A combination therapy approach was followed by encapsulating two chemotherapeutics, 5-Fluorouracil (5-Fu) and cyclophosphamide in poly(D, L-lactide-co-glycolide) (PLGA) microspheres. Magnetite nanoparticles and albumin were also incorporated in the microspheres to achieve targeted treatment. The microspheres were fabricated using oil-in-oil emulsion/solvent evaporation technique. Albumin is attracted to cancer cells and thus it is likely to draw the microspheres towards tumor cells. On application of magnetic field near tumor site, magnetites in the microspheres are likely to guide them to the region of magnetic field. This will allow release of drugs from microspheres in the cancer cells. Also the burst release of drugs and then slow release due to diffusion in the cancer cells lead to effective treatment and also limit excessive spreading of drugs in other regions of the body. Release rate study was carried out using high performance liquid chromatography (HPLC). Invitro and in-vivo study was carried out to check the efficacy of treatment.