The use of various pharmaceutical nanocarriers has become one of the most important areas of nanomedicine. Ideally, such carriers should be specifically delivered (targeted) to the pathological area to provide the maximum therapeutic efficacy. Among the many potential targets for such nanocarriers, tumors have been most often investigated. This review attempts to summarize currently available information regarding targeted pharmaceutical nanocarriers for cancer therapy and imaging. Certain issues related to some popular pharmaceutical nanocarriers, such as liposomes and polymeric micelles, are addressed, as are different ways to target tumors via specific ligands and via the stimuli sensitivity of the carriers. The importance of intracellular targeting of drug- and DNA-loaded pharmaceutical nanocarriers is specifically discussed, including intracellular delivery with cell-penetrating peptides.