Ocular drug delivery is one of the most attention-grabbing and challenging endeavors among the numerous existing drug delivery systems. From a drug delivery point of view, eye is an intricate organ to investigate and explore. In spite of many limitations, advancements have been made with the intention of improving the residence time or permeation of the drug in the ocular region. Poor bioavailability of topically administered drugs is the major issue pertaining to ocular drug delivery. Several efforts have been made towards improving precorneal residence time and corneal penetration, e.g. iontophoresis, prodrugs and ion-pairing, etc. Prodrug approach (chemical approach) has been explored by the formulation scientists to optimize the physicochemical and biochemical properties of drug molecules for improving ocular bioavailability. Formulation of ocular prodrugs is a challenging task as they should exhibit optimum chemical stability as well as enzymatic liability so that they are converted into parent drug after administration at the desired pace. This review will encompass the concept of derivatization and recent academic and industrial advancements in the field of ocular prodrugs. The progression in prodrug designing holds a potential future for ophthalmic drug delivery.