Magnetic microspheres hold great promise for reaching the goal of controlled and site specific drug delivery. Magnetic microspheres as an alternative to traditional radiation methods which uses highly penetrating radiations that is absorbed throughout the body. Its use is limited by toxicity and side effects. Now days, several targeted treatment systems including magnetic field, electric field, ultrasound, temperature, UV light and mechanical force are being used in many disease treatments (e.g. cancer, nerve damage, heart and artery, anti-diabetic, eye and other medical treatments). Among them, the magnetic targeted drug delivery system is one of the most attractive and promising strategy for delivering the drug to the specified site. Magnetically controlled drug targeting is one of the various possible ways of drug targeting. This technology is based on binding establish anticancer drug with ferrofluid that concentrate the drug in the area of interest (tumor site) by means of magnetic fields. There has been keen interest in the development of a magnetically target drug delivery system. These drug delivery systems aim to deliver the drug at a rate directed by the needs of the body during the period of treatment, and target the activity entity to the site of action. Magnetic microspheres were developed to overcome. CONCLUSION: Magnetism seems to be a common function of opening a new vista of a multi-barrier of multi-step drug delivery. Their main advantage is the targeting of drug using an external magnet, which can be accomplished very easily. They are relatively young drug delivery systems, having received attention from the early 1990s. In the early days of twentieth century, Paul Ehrlich envisioned his MAGIC BULLET CONCEPT-the idea that drugs reach the right site in the body, at the right time, at right concentration.