Liposomes and nanoparticles have emerged as versatile carrier systems for delivering active molecules in the organism. These colloidal particles have demonstrated enhanced efficacy compared to conventional drugs. However, the design of liposomes and nanoparticles with a prolonged circulation time and ability to deliver active compounds specifically to target sites remains an ongoing research goal. One interesting way to achieve active targeting is to attach ligands, such as monoclonal antibodies or peptides, to the carrier. These surface-bound ligands recognize and bind specifically to target cells. To this end, various techniques have been described, including covalent and noncovalent approaches. Both in vitro and in vivo studies have proved the efficacy of the concept of active targeting. The present review summarizes the most common coupling techniques developed for binding homing moieties to the surface of liposomes and nanoparticles. Various coupling methods, covalent and noncovalent, will be reviewed, with emphasis on the major differences between the coupling reactions, on their advantages and drawbacks, on the coupling efficiency obtained, and on the importance of combining active targeting with long-circulating particles.