4.7 Article

Development and Pharmacokinetics of a Novel Acetylsalicylic Acid Dry Powder for Pulmonary Administration

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PHARMACEUTICS
卷 14, 期 12, 页码 -

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MDPI
DOI: 10.3390/pharmaceutics14122819

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acetylsalycilic acid; aspirin; dry powders; inhalation; pulmonary delivery; pharmacokinetics

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This study developed a novel highly performing inhalable acetylsalicylic acid dry powder using nano spray-drying technique and leucine as an excipient. Compared with oral administration, the dry powder showed faster absorption in blood and higher retention in the lungs. The results suggest that this dry powder formulation has promising features for the treatment of inflammatory and infectious lung diseases.
Aspirin is an historic blockbuster product, and it has been proposed in a wide range of formulas. Due to exacerbation risks, the pulmonary route has been seldom considered as an alternative to conventional treatments. Only recently, owing to overt advantages, inhalable acetylsalicylic acid dry powders (ASA DPI) began to be considered as an option. In this work, we developed a novel highly performing inhalable ASA DPI using a nano spray-drying technique and leucine as an excipient and evaluated its pharmacokinetics compared with oral administration. The formulation obtained showed remarkable respirability and quality features. Serum and lung ASA DPI profiles showed faster presentation in blood and higher retention compared with oral administration. The dry powder was superior to the DPI suspension. The relative bioavailability in serum and lungs claimed superiority of ASA DPI over oral administration, notwithstanding a fourfold lower pulmonary dose. The obtained ASA DPI formulation shows promising features for the treatment of inflammatory and infectious lung pathologies.

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