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The development of lung cancer treatment has urged the delivery of chemotherapeutics and diagnostic agents to the lungs and their adjacent lymph nodes. The unavailability of a proper tool in current chemotherapy or diagnostic procedures leads to a lack of diagnosis at the early stage of lung cancer, which ultimately leads to it becoming the leading cause of cancer-related deaths worldwide. The introduction of dendrimers through the extension of nanotechnological research has brought a multifunctional nanotherapeutic or diagnostic system to the formulation scientists. Dendrimers contribute to encapsulation and solubilization of chemotherapeutics, active targeting via tunable surface properties, and passive targeting which leads to the development of suitable therapeutic and diagnostic tools in cancer treatment. This chapter provides a broad perspective of dendrimer-based tools in the treatment of lung cancer …