Efficacy Testing of Montelukast Loaded Large Porous Particles in Allergen-Induced Rat Asthma Model

Category
Regional Delivery: Challenges in Ocular Delivery and Pulmonary Delivery
Year
2013
Authors
Brijeshkumar Patel and Fakhrul Ahsan
Institutions
School of Pharmacy, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA
Summary

In this study, we investigated the efficacy of respirable large porous PLGA particles of montelukast in alleviating the symptoms of asthma in a rat model. PLGA particles of montelukast were prepared using a double emulsion-solvent evaporation method and the porosity was adjusted by incorporating polyethyleneimine (PEI), as a porosigen. Large porous particles (PEI-1) showed acceptable physicochemical properties and favorable release profiles for pulmonary administration. Compared to non-porous particles, PEI-1 showed reduced uptake by alveolar macrophages and increased deposition onto rat lungs. PEI-1 significantly reduced infiltration of inflammatory cells in the airways and narrowing of airway lumens in asthmatic rats. Overall, the preliminary data suggest that inhaled prolonged release montelukast particles could be used as an alternative to oral form of the drug.