With the aim of making specific targeting of silver nanoparticles as a drug for tumor cells and developing new anticancer agents, a novel nano-composite was developed. Albumin coated silver nanoparticles (ASNPs) were synthesized, and their anti-cancerous effects were evaluated against MDA-MB 231, a human breast cancer cell line. The synthesized ASNPs were characterized by spectroscopic methods. The morphological changes of the cells were observed by inverted, florescent microscopy and also by DNA ladder pattern on gel electrophoresis; the results revealed that the cell death process occurred through the apoptosis mechanism. It was found that ASNPs with a size of 90 nm and negatively charged with a zeta-potential of about −20 mV could be specifically taken up by tumor cells. The LD50 of ASNPs against MDA-MB 231 (5 μM), was found to be 30 times higher than that for white normal blood cells (152 μM). The characteristics of the synthesized ASNPs included; intact structure of coated albumin, higher cytotoxicity against cancer cells than over normal cells, and cell death based on apoptosis and reduction of gland tumor sizes in mice. This work indicates that ASNPs could be a good candidate for chemotherapeutic drug.