Millions of patients worldwide have benefited from technological innovation from biomaterials. Yet, while life expectancy continues to increase, organ failure and traumatic injury continue to fill hospitals and diminish the quality of life. Advances in understanding disease and tissue regeneration combined with increased accessibility of modern technology have created new opportunities for the use of biomaterials in unprecedented ways. Materials can now be rapidly created and selected to target specific cells, change shape in response to external stimulus, and instruct tissue regeneration. Here we describe a few of these technologies with emphasis on targeted drug delivery vehicles, high-throughput material synthesis, minimally invasive biodegradable shape-memory materials, and development of strategies to enhance tissue regeneration through delivery of instructive materials.