A number of novel drug delivery systems have emerged by various routes of administration, to achieve controlled and targeted drug delivery, magnetic drug delivery system being one of them which include magnetic microspheres, magnetic liposomes, magnetic nanoparticles, magnetic resealed erythrocytes, magnetic emulsion and others. Magnetic microspheres& molecular magnetic labels have been used for great number of application in various areas of biosciences, targeted drug delivery, imaging and in bioseparation technology. This review summarize about application of magnetism in targeted non invasive drug delivery system of magnetic microspheres. Over the years, magnetic drug delivery system have been investigated for targeted drug delivery especially magnetic targeted chemotherapy due to their better tumor targeting, therapeutic efficacy, lower toxicity and flexibility to be tailored for varied desirable purposes.