Prodrugs, the pharmacologically inactive derivatives of active drugs, are designed to maximize the amount of active drug that reaches its site of action, through manipulation of the physicochemical, biopharmaceutical or pharmacokinetic properties of the drug. But new developments are increasingly taking the concept beyond issues of availability to include targeting. The development of prodrugs promises to be very effective method for treatment of diseases in future. This approach has several advantages over conventional drug administration. In this mini review, prodrugs are discussed with a focus on the viability of the prodrug approach as a means of attaining targeted drug delivery. Next, several examples of where the prodrug approach has been used to achieve targeted delivery will be discussed.