Almost a century's dedicated research into micro‐ and nanomaterials has yielded fruitful development of preparation methods, achieving fine control over product properties among a broad spectrum of materials. One critical application of these materials lies within the healthcare sector for diagnostic, prophylactic, and therapeutic purposes. However, bench‐to‐bedside translations are still hindered by some unmet demands, especially the scaling‐up from lab‐scale preparation to industry‐level production. The current review recapitulates the strategies of micro‐ and nanomaterial preparation from a holistic viewpoint. The similarities in synthesis and processing methods for various types of materials are highlighted. Furthermore, patents of commercialized nanomedicines are revisited to reveal a solid progress of micro‐ and nanomanufacturing in the last decade. In conclusion, further interdisciplinary research between fields in materials manufacturing is beneficial for the clinical translation and eventually unleashing the power of materials at small dimensions.