This review provides an outline of the polymeric micro/nanostructured advanced systems that are suited for the controlled and targeted administration of, specifically, nonconventional drugs. The contribution of new trends in drug-delivery technology is focused on two major parts, dealing with brief surveys of: the biodegradable/bioerodible polymeric systems used in the formulation of micro/nanoparticles and techniques used in the preparation of micro/nanoparticles for their biomedical application in cancer treatment specifically, in inflammation pathologies, as oxygen carriers (blood substitutes) and in tissue-engineering practice. A small discussion of the future perspectives of the described systems is also given.