Prodrugs are bioreversible derivatives of drug molecules that undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug, which can then exert the desired pharmacological effect. Prodrug design is a choice of approach in solving many of the problems like stability, toxicity, solubility, permeability and drug targeting that affect drug discovery and development. Prodrug design is fruitful approach for drug targeting by changing the physiochemical, biopharmaceutical or pharmacokinetic properties of drugs. About 10-14% of drugs approved worldwide can be classified as prodrugs. The present article takes a review of introduction, classification, applications of prodrug design in various areas of drug development and basic functional groups that are amenable to prodrug design. Keywords: Prodrugs, objectives, classification, application, functional groups, limitation.
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