Abstract: Non-steroidal anti-inflammatory drugs are the most commonly used and widely prescribed drugs all over the world. With the wide advantages they are also associated with severe Gastro-Intestinal side effects. Developments of novel drug delivery systems have always been a challenge to formulation scientists because of their high instability and economic factor compared to the conventional dosage forms. Thus the main objective of the present investigation was to develop gelatin surface modified bovine serum albumin microspheres containing anti-arthritic drug and to evaluate its potential as targeted drug delivery system. Hence there is a prolonged release of the drug along with minimized side effects. A brief overview of the methods developed for the preparation of albumin microspheres and the most suitable techniques for optimum entrapment of drug is emphasized. The in-vitro evaluations are also explained. In order to appreciate the medical application possibilities of albumin microspheres in novel drug delivery, some fundamental aspects are also briefly discussed.