Formulation and evaluation of carrier-free dry powder inhaler containing sildenafil

Nguyen, Thi-Tram; Yi, Eun-Jin; Hwang, Kyu-Mok; Cho, Cheol-Hee; Park, Chun‐Woong; Kim, Ju‐Young; Rhee, Yun-Seok; Park, Eun-Seok

doi:10.1007/s13346-018-0586-5

Cited by 16 publications

(7 citation statements)

References 45 publications

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“…The delivery of dry powders to the lung has become a popular delivery system for both topical and systemic disease states, due to their large surface area, thin epithelial barrier, and rich blood supply [ 7 ]. Pulmonary delivery systems are classified into three types: DPIs, pressurized metered-dose inhalers (pMDIs), and nebulizer.…”

Section: Introductionmentioning

confidence: 99%

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

et al. 2020

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The purpose of this study was to prepare spray dried bosentan microparticles for dry powder inhaler and to characterize its physicochemical and aerodynamic properties. The microparticles were prepared from ethanol/water solutions containing bosentan using spray dryer. Three types of formulations (SD60, SD80, and SD100) depending on the various ethanol concentrations (60%, 80%, and 100%, respectively) were used. Bosentan microparticle formulations were characterized by scanning electron microscopy, powder X-ray diffraction, laser diffraction particle sizing, differential scanning calorimetry, Fourier-transform infrared spectroscopy, dissolution test, and in vitro aerodynamic performance using Andersen cascade impactor™ (ACI) system. In addition, particle image velocimetry (PIV) system was used for directly confirming the actual movement of the aerosolized particles. Bosentan microparticles resulted in formulations with various shapes, surface morphology, and particle size distributions. SD100 was a smooth surface with spherical morphology, SD80 was a rough surfaced with spherical morphology and SD60 was a rough surfaced with corrugated morphology. SD100, SD80, and SD60 showed significantly high drug release up to 1 h compared with raw bosentan. The aerodynamic size of SD80 and SD60 was 1.27 µm and SD100 was 6.95 µm. The microparticles with smaller particle size and a rough surface aerosolized better (%FPF: 63.07 ± 2.39 and 68.27 ± 8.99 for SD60 and SD80, respectively) than larger particle size and smooth surface microparticle (%FPF: 22.64 ± 11.50 for SD100).

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Section: Introductionmentioning

confidence: 99%

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

et al. 2020

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“…The formulation of carrier free dry powders can be achieved by a variety of methods. These include the formation of salts, such as the generation of a sildenafil-citrate salt [ 92 ], forming complexes with cationic groups, such as the generation of indomethacin and polylysine microparticles [ 89 ], and forming CASDs, such as with ciprofloxacin and colistin [ 101 ]. Another route being investigated is the generation of cocrystals and seems to be a promising method of improving physicochemical properties if other methods are not suitable.…”

Section: The Design Of Carrier Free Formulations Using Cocrystalsmentioning

confidence: 99%

Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions

et al. 2021

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It is well established that currently available inhaled drug formulations are associated with extremely low lung deposition. Currently available technologies alleviate this low deposition problem via mixing the drug with inert larger particles, such as lactose monohydrate. Those inert particles are retained in the inhalation device or impacted in the throat and swallowed, allowing the smaller drug particles to continue their journey towards the lungs. While this seems like a practical approach, in some formulations, the ratio between the carrier to drug particles can be as much as 30 to 1. This limitation becomes more critical when treating lung conditions that inherently require large doses of the drug, such as antibiotics and antivirals that treat lung infections and anticancer drugs. The focus of this review article is to review the recent advancements in carrier free technologies that are based on coamorphous solid dispersions and cocrystals that can improve flow properties, and help with delivering larger doses of the drug to the lungs.

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“…Therefore, to treat and prevent SARS-CoV-2 using NFM, it is necessary to administer the drug via the respiratory tract, which is one of the routes of viral invasion and has a lower esterase level than the blood [ 19 ]. When the drug is administered via the respiratory tract, it results in high efficacy and reduced incidence of side effects [ 20 , 21 , 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats

et al. 2021

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Coronavirus disease 2019 (COVID-19), caused by a new strain of coronavirus called severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is spreading rapidly worldwide. Nafamostat mesylate (NFM) suppresses transmembrane serine protease 2 and SARS-CoV-2 S protein-mediated fusion. In this study, pharmacokinetics and lung distribution of NFM, administered via intravenous and intratracheal routes, were determined using high performance liquid chromatography analysis of blood plasma, lung lumen using bronchoalveolar lavage fluid, and lung tissue. Intratracheal administration had higher drug delivery and longer residual time in the lung lumen and tissue, which are the main sites of action, than intravenous administration. We confirmed the effect of lecithin as a stabilizer through an ex vivo stability test. Lecithin acts as an inhibitor of carboxylesterase and delays NFM decomposition. We prepared inhalable microparticles with NFM, lecithin, and mannitol via the co-spray method. The formulation prepared using an NFM:lecithin:mannitol ratio of 1:1:100 had a small particle size and excellent aerodynamic performance. Spray dried microparticles containing NFM, lecithin, and mannitol (1:1:100) had the longest residual time in the lung tissue. In conclusion, NFM-inhalable microparticles were prepared and confirmed to be delivered into the respiratory tract, such as lung lumen and lung tissue, through in vitro and in vivo evaluations.

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Formulation and evaluation of carrier-free dry powder inhaler containing sildenafil

Cited by 16 publications

References 45 publications

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

Pulmonary Drug Delivery of Antimicrobials and Anticancer Drugs Using Solid Dispersions

Co-Spray Dried Nafamostat Mesylate with Lecithin and Mannitol as Respirable Microparticles for Targeted Pulmonary Delivery: Pharmacokinetics and Lung Distribution in Rats

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