Abstract: Lung cancer has become the malignant tumor with the highest incidence and mortality rates in China. Commonly used anticancer drugs can no longer meet the clinical demand. Natural drug components have been an important source for the development and screening of new anticancer drugs because of their remarkable efficacy and high safety in the treatment of lung cancer, but some of them are characterized by poor water solubility, low bioavailability, poor stability, and non-specific distribution. In recent years, new active targeted drug delivery systems loaded with natural drug components have gradually emerged, overcoming the many shortcomings of natural drug components and achieving remarkable efficacy in lung cancer treatment. This paper provides a summary of relevant active targeted drug delivery systems from two perspectives: targeting tumor cell surface receptors and targeting the tumor microenvironment, which may provide references for drug development and clinical application in the treatment of lung cancer.