Chronic obstructive pulmonary disease (COPD), characterized by airway inflammation and progressive airflow limitation, is one of the leading causes of mortality worldwide. Bronchodilators, corticosteroids, or antibiotics are used for treatment of COPD, but the drugs are not delivered properly to the target cells or a tissue, which remains a challenge. Nanoparticles (NPs) have gained a tremendous interest in respiratory medicine due to their smaller size, higher surface to volume ratio, and advantages such as targeting effects, patient compliance, and improved pharmacotherapy. Sustained delivery of drugs mediated by NPs to the targeted site is needed to control cell chemotaxis, fibrosis, and chronic obstruction of lungs in COPD. Development of multifunctional biodegradable NPs that are nontoxic and can help in overcoming airway defense will be beneficial in future for COPD.