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The conversion of novel therapeutics into medicines is frequently delayed by the lack of parallel investment in the ‘enabling' field of drug delivery. During the past few years, a large number of new drug delivery technologies have been optimized to guide the potential drug specifically to the target where it is needed and to deliver it at an effective concentration and at the correct time, with safety and reproducibility. In this article, the use of micro- and nanosystems, pulsatile drug delivery systems, macromolecular conjugation and microfabricated systems together with their application in preclinical or clinical investigation will be discussed.