Spray-dried indomethacin microparticles designed for asthma inhalatory treatments

NAZARETH E. CESCHAN; MARÍA PAULA CALDAROLA; VERÓNICA BUCALÁ; JUAN MANUEL FIGUEROA; ANDREA V. DUGOUR; M. VERÓNICA RAMÍREZ RIGO

Virtual

Congreso; VI Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2020+1); 2021

Universidad Nacional de Córdoba y Universidad Nacional de Rosario

Indomethacin (IN), has demonstrated usefulness for treating bronchial inflammatory asthma responses. In the frame of a dry powder inhaler development, IN microparticles (MPIN) were produced by spray-drying. The study aim was: (a) evaluating the effect of spray-drying operating variables on MPIN aerodynamic properties and (b) measuring the effect of MPIN administation in Calu-3 cell line interleukins IL-6 and IL-8 production. IN dissolved in ethanol (1 % W/V) was processed in a lab-scale equipment using a high-performance cyclone to collect MPIN. Liquid feed flow-rate (Qli, 1.5 and 3 mL/min), atomization air flow-rate (Qaa, 450 and 742 L/h) and aspiration (A, 90 and 100 %) varied to assess their impact on aerodynamic parameters, that were studied in a cascade impactor, using a high-resistant inhaler. For cell culture studies, different MPIN concentrations (20 and 50 mM) were added to Calu-3 cell-line. The highest fine particle fraction for particles with aerodynamic diameters <5 μm (35.82 %) and the lowest mass median aerodynamic diameter (3.60 μm) values were found for Qaa: 450 L/h; A: 90 % and Qli: 3 mL/min spray-drying operating variables. MPIN significantly reduced IL-6 and IL-8 production in Calu-3 cells. No statistical significant differences were found between concentrations assayed. MPIN produced under the selected spray-drying conditions are a promising system for athsma inhalatory treatments.