This chapter explores the integration of nanotechnology and biocatalysis, with a focus on nanobiocatalysts—enzymatic systems enhanced by nanomaterials. It outlines fundamental concepts, development strategies, and applications in pharmaceutical production, while also emphasizing the role of nanoscaffolds in advancing catalytic performance. The chapter examines future trends, including the integration of artificial intelligence and Internet of Things technologies for process optimization. Nanobiocatalysts offer distinct advantages such as improved stability, reusability, enhanced catalytic activity, and the creation of efficient multi-enzyme systems. By showcasing their highly specific and environmentally friendly catalytic capabilities, the chapter highlights how these systems are transforming industries, particularly pharmaceuticals.