Applicability of an ultrasonic nebulization system for the airways delivery of beclomethasone dipropionate in a murine model of asthma.

PURPOSE: We have assessed the use of an ultrasonic nebulization system (UNS), composed of ultrasonic nebulizer and diffusion dryer filled with charcoal, for the effective delivery of beclomethasone to the airways in a murine asthma model. METHODS: Solution of beclomethasone in ethanol was aerosolized using an ultrasonic nebulizer. Passage of the aerosol through a drying column containing charcoal and deionizer produced dry beclomethasone particles. Particles were delivered to BALB/c mice placed in a whole-body exposition chamber 1 h before intranasal challenge with ovalbumine. Efficacy of beclomethasone delivery was evaluated by examining bronchoalveolar lavage fluid (BALF) cytology. RESULTS: Effect of three UNS system parameters on aerosol particle size was investigated. The critical parameter affecting the size of dry particles was beclomethasone concentration in aerosolized solution and solution flow rate while power level of ultrasonic nebulizer generator had no effect. Administration of beclomethasone at calculated dose of 150 microg/kg to mice significantly decreased total cell number and relative eosinophil number in BALF. CONCLUSIONS: The UNS system produces a monodisperse aerosol that can be used for inhalative delivery of poorly water soluble substances to experimental animals. The UNS system minimizes formulation requirements and allows rapid and relatively simple efficacy and toxicity testing in animals.

Solid-state investigation of piroxicam benzoate.

Solid-state properties of piroxicam benzoate, an ester prodrug of piroxicam, were investigated. Samples were prepared by recrystallization from various organic solvents (toluene, ethanol, methanol, ethyl acetate and acetone). Recrystallized samples were characterized by means of FTIR, DSC, TGA, SEM and XRPD. DSC, TGA and XRPD methods confirmed that piroxicam benzoate crystallized in two pseudopolymorphic forms, A and B. Pseudopolymorphic form A was obtained by recrystallization from ethanol and methanol by slow cooling at room temperature and by rapid cooling in an ice-cold bath, and also from toluene by rapid cooling in an ice-cold bath. Pseudopolymorphic form B was obtained by recrystallization from toluene by slow cooling at room temperature.