Multifunctional Nanocarrier Drug Delivery Systems: From Diverse Design to Precise Biomedical Applications

Abstract Due to the high complexity of the disease mechanisms, rendering conventional single‐target symptomatic therapies are increasingly inadequate to meet evolving clinical demands. Multifunctional nanocarrier drug delivery systems (MNDDS) with precision targeting and tunable functionalities have emerged as a revolutionary strategy to address current therapeutic limitations. MNDDS enables spatiotemporally controlled drug delivery and customizable therapeutic outcomes, thereby serving as a cornerstone for advancing precision medicine. To systematically survey the latest advancements in MNDDS and facilitate cross‐disciplinary innovation, this review begins by classifying carrier platforms into biological and non‐biological categories based on their constituent materials. Then, the integration of diverse therapeutic payloads, encompassing chemical agents, protein/peptide therapeutics, nucleic acid‐based drugs, and other bioactive compounds are summarized. Following, engineering strategies are elaborated for achieving active targeting and passive targeting through systematic structural and surface modifications. Furthermore, the applications of MNDDS for disease treatment are highlighted. Finally, emerging strategies integrating intelligent bioinspired carrier design, dynamic smart materials, and personalized microenvironment engineering that hold transformative potential to bridge the gap from lesion‐specific targeting to real‐time theranostics are foregrounded. It is believed that this review can inspire multidisciplinary collaboration and accelerate the development of next‐generation MNDDS.