Starch has cropped up as a new attractive biopolymer for use in pharmaceutical applications, owing to its distinctive physical, chemical and functional properties. This biopolymer has a number of potential advantages like being biocompatible, low cost, easily isolated from plant sources and non-toxic in nature. In the field of pharmaceutical science, starch is used as a raw material for the development of various drug delivery platforms. Generally, cassava starch (tapioca) is obtained from swollen roots of the perennial shrub Manihot esculenta and it contains a low amount of amylose in contrast to other varieties of starches. Because of this reason, cassava starch exhibits various prime benefits including little gelatinization temperature, higher swelling power and produces relatively high viscosity paste, making it preferable as an excipient for pharmaceutical applications. However, cassava starches in their native form are offensive for many applications due to their inefficiency to withstand various processing requirements like high temperature and diverse pH, but their use is enhanced by starch modification. These functional starches have demonstrated outstanding potential as primary excipients in a number of pharmaceutical formulations. In this article, we discuss the potential application of cassava starches in the pharmaceutical and biomedical fields along with the toxicity assessment of modified cassava starches.