This article reviews the developmental stages and strategies used to assess the biomedical utility of biopolymer albumin from the 1970s to early 2002. The basic method and mechanism(s) of preparation of albumin microspheres and subsequent modifications made to overcome the drawbacks of earlier approaches and the need for further developments are discussed, as are the processing parameters and the level of various ingredients affecting the physicochemical properties of the albumin microspheres. Different equations proposed by various investigators to modulate in vitro release kinetics are reviewed. The microscopic structural and surface properties, the chemical modification of the biopolymer (e.g., cationization, tagging with amino acids and sugar moieties) for tissue specificity or to influence the release profile and biodegradation are discussed. An array of potential diagnostic applications and the use of albumin microspheres as a drug delivery system are reviewed. Drug Dev.