Abstract
Most of the marketed dry powder inhalation (DPI) products are traditional, carrier-based formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new formulation, confirming that the interparticle interactions were changed favorably.
Highlights
The delivery of active pharmaceutical ingredients (APIs) via the lung allows the treatment of several local and systemic diseases
It can be concluded that in the case of a traditional, carrier-based system, after the surface treatment with magnesium stearate (MgSt), the carrier particles did not show much improvement in the in vitro dissolution results, and the interactive physical blend of the spray-dried drug—micronized (μMXP) and the spray-dried (MXPspd)—with the untreated carrier particles did not represent a definite improvement over the results of the MXPspd considering the in vitro and in silico data
The study shows that among the developed and innovative, carrier-based systems, the MXPspd + IH70_MgSt formulation had the most outstanding in vitro lung deposition results—fine particle fraction (FPF) < 5 μm (72.32%) and FPF < 3 μm (46.05%)—which was supported by in silico measurements and predicted by physical examinations
Summary
The delivery of active pharmaceutical ingredients (APIs) via the lung allows the treatment of several local (e.g., cystic fibrosis—CF—and chronic obstructive pulmonary disease—COPD) and systemic diseases (e.g., diabetes mellitus and agitation associated with schizophrenia). This possibility can be explained by the fact that the lung has highly absorptive tissue with a large surface area, which has a thin adsorption membrane and excellent blood supply. The traditional, carrier-based dry powder inhalers (DPIs) are the most widely used formulations in this therapy, which means an interactive physical mixture of large carrier particles and particle size-optimized drugs [5,6]. It should be noted that the carrier-based DPI formulations still have only 20–30% of the fine particle fraction (FPF) values [8]
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