Ideally a drug should be administered in a form that it exerts its pharmacological action at the target site using the lowest concentration possible and without undesirable effects. Drug targeting is the approach which is followed for the purpose. Among different approaches preparation of synthetic glycosides of target drug and administering them orally is one of the most recent approaches. The drug glycoside on reaching colonic region releases the active drug through enzymatic action. This approach has been detailed with different successful examples. Synthetic drug-glycosides, besides being used as drug targeting agents, have been shown to exhibit varied biological activities such as antineoplastic, antidiabetic, antiinfllamatory etc., which have been reviewed. Synthetic approaches to O-, C-, N-, S glycosides have been discussed.