Formulation development and in-vitro evaluation of montelukast sodium pressurized metered dose inhaler

Nanotechnology-Assisted Metered-Dose Inhalers (MDIs) for High-Performance Pulmonary Drug Delivery Applications

“…However, NR8383 cells incubated with a pre-mixed propellant showed significantly higher nitric oxide (NO) quantities than NR8383 cells incubated with a single HFA propellant. Briefly, the montelukast pMDI are non-toxic and are not expected to aggravate airway cells but, further in-vivo investigations are essential to conclude the safety of montelukast pMDI formulations ( 107 ).…”

The pulmonary route as a way to drug repositioning in COVID-19 therapy

“…however, it shows that the formulation did not present toxicity to macrophages in the pulmonary airways of rats or in human lung cells. [ 68 ] Estradiol DPI Porous MP by SD Albumin, lactose and DPPC N/I 4,1 10,1 32,87 - N/I In Wistar rats, 600 μg dosages showed a bioavailability of 86% and high drug systemic concentration for 5 days. 0,6 The high values ​​of average geometric diameter and the low mass density of the formulations favoured the efficient entry of particles into the lungs and the prolonged release of the drug into the systemic circulation.…”

“…Due to the lower expression of cytochrome P450 3A4 enzyme in the lungs [ 66 ], when MLK is administered via pulmonary route its metabolization is reduced compared to the liver [ 67 ]. So, the pulmonary route can improves its bioavailability [ 68 ] in comparison with the oral route, for which is approximately 64%, due to the first pass effect [ 46 , 69 70 ]. As MLK is used for asthma treatment, there are plenty of investigations for its pulmonary administration.…”

“…Probably, because of that, 6 of 8 studies with MLK presented in vivo experimental data ( Table 2 ). The majority uses DPI, as microparticles, but it was also possible to find one study with pressurized metered-dose inhaler (pMDI) ( Table 2 ) [ 68 ]. The SD technique was widely used and several strategies were applied to increase drug release and reach the deep lung, such as porous particles [ 67 , 71 ].…”

“… Drug Number of studies Formulation Spray-drying Microparticles Parameters Ref. DPI Solution/suspension for nebulization Particle size FPF FR In vitro assays In vivo assays Dosage Doxycycline 6 4 1 4 5 3 5 0 3 1 1 [ [58] , [59] , [60] , [61] , [62] , 72 ] Estradiol 3 3 0 3 3 1 2 2 0 1 0 [ 63 , 78 , 81 ] Montelukast 8 7 0 3 7 6 5 3 5 6 4 [ 46 , 68 , 71 , [73] , [74] , [75] …”