The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with poor water solubility. Issues associated with poor solubility can lead to low bioavailability, resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly watersoluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water-soluble drugs can be achieved. In fact, numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products, and several marketed drugs have been reformulated to improve efficacy, safety, and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies.