Formulation and evaluation of dry powder inhaler of Ketotifen

Abstract

Asthma is a chronic inflammatory disease of the airways. Ketotifen is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer and prevents the release of inflammatory mediators. Orally in the treatment and prevention of asthma and other allergic attacks are used. However to avoid the side effects of oral administration, inhaled formulation of ketotifen is formulated. Dry powder inhalation is a potent alternative route for drug administration. Aim The present study was designed to prepare microparticles for pulmonary drug delivery of ketotifen. Methods Particle engineering for pulmonary drug delivery can be done by changing spray drying conditions. Size and size distribution, morphology and crystallinity of particles were evaluated by laser scanning electron microscopy (SEM) and differential scanning calorimetry (DSC) methods, respectively. The aerosolization efficiency and aerodynamic properties of dry powders were determined by next generation impactor (NGI). Results Ethanol and Water are considered as the main solvent of ketotifen. Formulated microparticles with porous and low density structure creates proper situation for pulmonary purposes. High FPF and other acceptable criteriaes also show that these particles can be used as dry powder inhalers. The particle improve the medication therapy because few amounts of medicine will be needed, so the side effets reduce. Discussion

SEM images showed microparticles in the suitable range, shape and Surface characteristics for pulmonary drug delivery. Aerosolization evaluation of spray dried formulations with different concentration and feed solution and also change of solvent type, indicated that formulations showed the best aerosolization efficiency ,fine particle fraction (FPF), mass median aerodynamical diameter (MMAD) and also with suitable morphology and DSC thermogram .