Lung cancer (LC) is the largest cause of cancer mortality, accounting for around 18.4% of all cancer deaths in both sexes combined. One of the key treatments for LC is the use of systemic medicines. However, the therapeutic efficacy of these medications is restricted because to the significant side effects, systemic toxicity, and poor selectivity associated with them. In contrast, pulmonary anticancer medication administration has several advantages over traditional routes. The inhalation method allows for the direct delivery of chemotherapeutic drugs to the target LC cells, which may boost antitumor effectiveness and lead to reduced dose and fewer systemic effects. Nonetheless, this method has numerous physiological and technological obstacles that may have a major impact on lung deposition, retention, and efficacy. Phytochemicals, or naturally occurring plant molecules, are important sources for new medications and are also used to treat cancer. Taxol analogues, vinca alkaloids like vincristine and vinblastine, and analogues of podophyllotoxin are a few typical examples. These phytochemicals frequently work by controlling molecular pathways that are connected to the development and spread of cancer. The precise processes include boosting antioxidant status, neutralizing carcinogens, reducing proliferation, inducing cell cycle arrest and apoptosis, and immune system control.