The use of nanoparticles in cancer therapy is attractive for several reasons: they exhibit unique pharmacokinetics, including minimal renal filtration; they have high surface-to-volume ratios enabling modification with various surface functional groups that home, internalize, or stabilize; and they may be constructed from a wide range of materials used to encapsulate or solubilize therapeutic agents for drug delivery or to provide unique optical, magnetic, and electrical properties for imaging and remote actuation. The topology of a nanoparticle—core, coating, and surface functional groups—makes it particularly amenable to modular design, whereby features and functional moieties may be interchanged or combined. Although many functionalities of nanopar-ticles have been demonstrated, including some clinically approved drug formulations and imaging agents,3,8 the consolidation of these into multifunctional nanoparticles capable of targeting, imaging, and delivering therapeutics is an exciting area of research that holds great promise for cancer therapy in the future.

Figure 5.11 schematically depicts a hypothetical multifunctional particle that has been engineered to include many features such as the ability to target tumors, evade uptake by the reticuloendothelial system (RES), protect therapeutics that can be released on demand, act as sensors of tumor responsiveness, and provide image contrast to visualize sites of disease and monitor disease progression. Some of these features, such as targeting, leverage biological machinery. Others are derived synthetically and enable external probing or manipulation that is otherwise not feasible in biological systems. In this chapter, we review both bio-inspired and synthetic nanoparticle functionalities that have been used in cancer therapy and address both current efforts and future opportunities to combine these into multifunctional devices.

FIGURE 5.1 Schematic depiction of a multifunctional nanoparticle. A hypothetical nanoparticle targets the tumor, senses and reports molecular signatures, and delivers a therapeutic in response to an external or biological trigger. (From Ruoslahti, E., Cancer Cell, 2, 97-98, 2002.)
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