This is the peer-reviewed version of the book chapter Stevanović, M., 2017. Chapter 11 -Polymeric micro-and nanoparticles for controlled and targeted drug delivery, in: Andronescu, E., Grumezescu, A.M. (Eds.), Nanostructures for Drug Delivery, Micro and Nano Technologies. Elsevier, pp. 355-378. https://doi.Nanotechnology, among others, has great potential in the field of medicine and pharmacy because nanoobjects have comparable dimensions to biological entities. Polymer-based particles play an integral role as vehicles in the controlled delivery of different forms and types of active substances, such as anticancer drugs, antihypertensive and immunomodulatory agents, medical imaging contrast media, hormones, vitamins and different macromolecules, such as nucleic acids (deoxyribonucleic acid, ribonucleic acid), proteins, antibodies, etc. The release of the active agent may be constant over a long period, it may be cyclic over a long period, or it may be triggered by the environment or other external events. The purpose behind controlling the drug delivery is to achieve more effective therapies while eliminating the potential for both under-and overdosing. Other benefits of using controlled-delivery systems can include the maintenance of drug levels within a desired range, the need for fewer administrations, optimal use of the drug in question, and increased patient compliance. This review article reports on obtaining polymeric micro and nanoparticles with special emphasis on obtaining polyester particles, incorporation of different active substances within polymer matrix, degradation and release process of active substances from the polymeric particles, physiochemical and biological properties of such obtained systems, as well as about their application as drug delivery systems.