During the last few decades, a fair amount of scientific investigation has focused on developing novel and efficient drug delivery systems. According to different clinical needs, specific biopharmaceutical carriers have been proposed. Micro-and nanoparticulated systems, membranes and films, gels and even microelectronic chips have been successfully applied in order to deliver biopharmaceuticals via different anatomical routes. The ultimate goal is to deliver the potential drugs to target tissues, where regeneration or therapies (chemotherapy, antibiotics, and analgesics) are needed. Thereby, the bioactive molecule should be protected against environmental degradation. Delivery should be achieved in a dose-and time-correct manner. Drug delivery systems (DDS) have been conceived to provide improvements in drug administration such as ability to enhance the stability, absorption and therapeutic concentration of the molecules in combination with a long-term and controlled release of the drug. Moreover, the adverse effects related with some drugs can be reduced, and patient compliance could be improved. Recent advances in biotechnology, pharmaceutical sciences, molecular biology, polymer chemistry and nanotechnology are now opening up exciting possibilities in the field of DDS. However, it is also recognized that there are several key obstacles to overcome in bringing such approaches into routine clinical use. This review describes the present state-of-the-art DDS, with examples of current clinical applications, and the promises and challenges for the future in this innovative field.