Chemotherapy at present remains the main form of treatment for cancer, though there is no clinically available antineoplastic drug that acts selectively on the tumor mass. For this reason, the scientific research is focused towards the development of novel cancer therapies and drug delivery strategies, like drug targeting, that would enhance the therapeutic efficacy of drugs while reducing their side toxicity. This review describes tree types of nanoparticles used in active targeting for cancer treatment: liposomes, lipid and polymer nanoparticles, and micelles. The opportunities and challenges achieved by the proposed strategies of active targeting have been highlighted, as well as the necessity to conciliate the targeting efficiency of drug nanocarriers with their longevity in the bloodstream.