Targeted delivery of anticancer drugs is one of the most actively pursued goals in anticancer chemotherapy. A major disadvantage of anticancer drugs is their lack of selectivity for tumor tissue, which causes severe side effects and results in low cure rates. Any strategy by which a cytotoxic drug is targeted to the tumor, thus increasing the therapeutic index of the drug, is a way of improving cancer chemotherapy and minimizing systematic toxicity. This study covers the preparation of the gelatin microsphere (GM)- albumin (BSA) conjugate for the development of a "drug targeting" approach in cancer therapy. Gelatin microspheres of 5% (w/v) gelatin content were prepared by crosslinking with glutaraldehyde (GTA) at 0.5% (v/v) concentration. The particle size and morphology of microspheres were analyzed by Particle Size Analyzer and Scanning Electron Microscopy (SEM). Gelatin micospheres were chemically conjugated to bovine serum albumin in PBS (0.01M, pH 7.4) at 4degreesC. The solution was then filtered and the GM-BSA conjugates were vacuum dried. The activity of BSA conjugated to GM was tested by using Immunodiffusion Techniques. The percent antigen-antibody binding between BSA and anti-BSA was evaluated by measuring the band widths of precipitates formed in the agar medium.