Oral modified-release multiple-unit dosage forms have always been more effective therapeutic alternative to conventional or immediate release single-unit dosage forms. With regards to the final dosage form, the multiparticulates are usually formulated into microspheres and filling them into hard gelatin capsules.Microspheres received much attention not only for prolonged release, but also for targeting of drugs. In future microspheres will find the central place in novel drug delivery, particularly in diseased cell sorting, diagnostics, genetic materials, targeted and effective drug delivery. Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers having a particle size ranging from 1-1000 μm. The range of Techniques for the preparation of microspheres offers a Variety of opportunities to control aspects of drug administration and enhance the therapeutic efficacy of a given drug. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microspheres as carriers for drugs also known as microparticles. It is the reliable means to deliver the drug to the target site with specificity, if modified, and to maintain the desired concentration at the site of interest. Microspheres received much attention not only for prolonged release, but also for targeting of anticancer drugs. In future by combining various other strategies, microspheres will find the central place in novel drug delivery, particularly in diseased cell sorting, diagnostics, gene & genetic materials, safe, targeted and effective in vivo delivery and supplements as miniature versions of diseased organ and tissues in the body.