Ketorolac tromethamine (KT) is a non-steroidal anti-inflammatory drug that belongs to the class of heteroaryl acetic acid derivatives. It is a non-selective cyclooxygenase (COX) inhibitor, being marketed in the racemate form. Most of its analgesic and COX inhibitory activity is retained in the S-isomer. Ketorolac is administered as its tromethamine salt orally, intramuscularly, intravenously and as a topical ophthalmic solution. The frequent occurrence of gastrointestinal disturbances including gastrointestinal bleeding, perforation and peptic ulceration along with the short mean plasma half-life (t(1/2) approximately 5.5 h) has prompted for the development of various formulation strategies for the appropriate delivery of KT. The article gives an overview of the main concepts used thus far to design various pharmaceutical dosage forms for the therapeutically effective delivery of the drug candidate through various routes. At present, a great deal of emphasis is being placed on the development of sustained release forms for the drug as this would aid in achieving the required therapeutic efficacy and better tolerance with fewer gastrointestinal side effects.