The interplay between cancer and inflammation has been well documented over the years and the role of nanomedical technologies for treating both these diseases has become evident over the past few decades. With the advances in nanoparticle-based imaging and therapeutic platforms that can exploit the pathological conditions of the tumor and the inflamed sites to effectively deliver drugs, genes and imaging/contrast agents; the management of such conditions with favorable therapeutic outcomes seems plausible. This review will summarize some of the latest advances in the field of targeted nanomedicine development to combat cancer and inflammation. Illustrative examples of multifunctional-targeted nanosystems are presented that highlight their potential in delivering diverse payloads, including small molecule drugs, nucleic acids and imaging agents for simultaneous theranostic interventions.