The number of cancer patients in the world is constantly increasing and it is considered as one of the deadliest among other diseases. There are urgent needs of effective and efficient medicine for late-stage cancer since none of current treatment has promising outcome especially related chemotherapy's side effects. Magnetic nanoparticles with its ability to be modified, coated and functionalized is a candidate for drug delivery's targeting carrier. This research goal was proposing a novel drug carrier to specifically target cancer cells without any significant remnant in other tissues. Our method begun with MNP coating using bovine serum albumin then functionalized with folic acid as targeting agent. Multiple evaluations towards functionalized MNP includes: MTT Assay for its toxicity, in vivo test for targeting capability assessment, and histopathology test for host's cellular response. The results showed that the magnetic nanoparticles-FA functionalized was non-toxic, no significant cellular damage, and it had a promising result to be used for further cancer targeting study.