Peucedanum praeruptorum Dunn has long been used in traditional Chinese medicine (TCM) for the treatment of respiratory diseases, its active constituent praeruptorin A (PA) has multiple anti-inflammatory activities. However, its bioavailability and therapeutic effect is not satisfactory in clinic owing to many physicochemical and physiologic barriers. Herein, this work highlights the successful development of an inhalable PA dry powder (MIL-100(Fe)-PA), which is facilely constructed through the optimization of the formulation between PA and a metal-organic framework (MIL-100(Fe)) carrier. Moderate pore and particle size distribution endow the dry powder with excellent loading efficiency and resistance to degradation. All ingredients and their interactions endow MIL-100(Fe)-PA favorable flowability, and pulmonary deposition, as well as direct lung drug delivery and release. These attractive characteristics enable the dry powder to effectively enhance alveolar epithelial cell penetration, improve anti-inflammatory activity, promote lung accumulation, and reduce the side effects of PA. Thus, this PA dry powder may open a new avenue for the inhalation treatment of diseases, greatly advancing its clinical application.