Cancer is not one disease but many. In fact, cancer is a collection of more than 100 different diseases. Cancer is the second leading cause of death in the United States with an estimated 1.7 million new cases expected in 2017 and approximately 600,000 Americans expected to succumb to the disease. While modern chemotherapeutics have provided considerable improvement to patient outcomes, we have yet to develop the "ideal" treatment for cancer. The medical community has long sought the ideal therapeutic – in fact Paul Ehrlich originally coined the concept of the "magic bullet" in the late 1800’s. Nanomedicine is a burgeoning field which can impact nearly every avenue of modern chemotherapeutics. Coupled with biological targeting agents, synthetic nanomaterials have the potential to render Ehrlich’s "magic bullet" concept a reality. In the first part of this thesis we have developed a new bioconjugation platform, and have applied this technology to the functionalization of nanoparticles (NPs). This platform is unique having; high water solubility, an inherent chromophore for quantification, and is chemically diverse. Further, we have shown that this platform can be utilized in the chemoselective reaction of nucleophilic amines. In the second part of the thesis we have constructed polyester based nanomaterials composed of poly(lactic-co-glycolic acid) (PLGA) and polycaprolactone (PCL). These nanomaterials were then adorned with a MUC1 specific antibody - TAB004 - and were shown to selectively accumulate at tumor sites in pancreatic cancers in vivo.