Passive and active targeted nanoparticulate delivery systems show promise to compensate for lacking properties of conventional therapy such as side effects, insufficient efficiency and accumulation of the drug at target site, poor pharmacokinetic properties etc. For active targeting, physically or covalently conjugated ligands, including monoclonal antibodies and their fragments, are consistently used and researched for targeting delivery systems or drugs to their target site. Currently, there are several FDA approved actively targeted antibody-drug conjugates, whereas no active targeted delivery system is in clinical use at present. However, efforts to successfully formulate actively targeted delivery systems continue. The scope of this review will be the use of monoclonal antibodies and their fragments as targeting ligands. General information about targeted delivery and antibodies will be given at the first half of the review. As for the second half, fragmentation of antibodies and conjugation approaches will be explained. Monoclonal antibodies and their fragments as targeting ligands and approaches for conjugating these ligands to nanoparticulate delivery systems and drugs will be the main focus of this review, polyclonal antibodies will not be included.