Optimization of a dry powder inhaler of ciprofloxacin-loaded polymeric nanomicelles by spray drying process

2019 ◽  
Vol 24 (5) ◽  
pp. 584-592 ◽  
Author(s):  
Mahdieh Farhangi ◽  
Arash Mahboubi ◽  
Farzad Kobarfard ◽  
Alireza Vatanara ◽  
Seyed Alireza Mortazavi
Drug Research ◽  
2019 ◽  
Vol 70 (01) ◽  
pp. 26-32
Author(s):  
Fariba Azari ◽  
Saeed Ghanbarzadeh ◽  
Rezvan Safdari ◽  
Shadi Yaqoubi ◽  
Khosro Adibkia ◽  
...  

Abstract Background Pulmonary drug delivery route is gaining much attention because it enables to target the active ingredients directly to lung both for local and systemic treatments, which maximize the therapeutic effect and minimize unwanted systemic toxicity. Dry powder inhaler (DPI) systems for asthma therapy have shown several merits to the other pulmonary delivery systems such as nebulizers and metered dose inhalers. Purpose The present study aims to develop and optimize a DPI formulation for Ketotifen fumarate through spray drying technique. Methods Particles size and morphology, crystallinity, and drug-excipient interaction of fabricated DPI formulations were evaluated by scanning electron microscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier Transform Infrared Spectroscopy methods, respectively. The aerosolization indexes and aerodynamic properties of dry powders were determined by next generation impactor. The powder flowability was assessed by measuring the Hausner ratio and compressibility index. Results Among solvent systems, ethanol-water mixture produced the most desirable powder property for inhalation after spray drying. Although co-spray dried formulations with ammonium bicarbonate resulted in the porous structure, it was not beneficial for DPI formulations due to the interaction with Ketotifen. DSC and XRD experiments proved the amorphous structure of prepared powders, which were stable for 12 months. Conclusion The results of this study demonstrate the potential of Ketotifen DPI formulation and pave a way to use it easily in an industrial scale.


2019 ◽  
Vol 14 (3) ◽  
pp. 239-260
Author(s):  
Vaishali Thakkar ◽  
Ekta Pandey ◽  
Tosha Pandya ◽  
Purvi Shah ◽  
Asha Patel ◽  
...  

Background: Targeting anti-tubercular therapeutics to alveolar macrophages using microparticles technology mainly focuses on increasing local concentrations of therapeutics and potentially reducing the frequency of dosing requirements. Rifampicin (RIF), Ofloxacin (OFX) and Ethambutol (ETH) combination show synergism. Objective: In light of the above facts, the focus of the present study was to develop and characterize novel Dry powder Inhaler formulation incorporating novel drug combination as a pulmonary delivery for the effective eradication of Tuberculosis. Method: Biodegradable microparticles containing RIF, OFX and ETH were prepared by a spray drying technique using PLGA polymer through the critical process as well as polymer attributes were screened and optimized using 23 factorial design. The identified critical process parameters (CPP’s) viz. Inlet temperature, Aspiration rate, and feed rate were selected as independent variables while percentage yield, percentage entrapment efficiency, and particle size were selected as a response. The formulated microparticles were evaluated for particle size, drug-polymer compatibility study, aerodynamic behavior, morphology, particle size distribution, crystallinity, residual solvent content, in-vitro drug release study, and stability study. Results: By choosing the optimum spray drying conditions maximum yield of 73%, entrapment efficiency of 86% and particle size of 1.4 μm was attained of the optimized batch. Thus the results revealed that spherical microparticles are suitable for inhalation and sustained release for 12 h. Conclusion: The successful formulation and evaluation of dry powder could be used as an enhanced therapeutic alternative of the standard oral anti-tubercular regimen, rescuing oral dosing, shortening drug regimen and limiting toxicity. This will ultimately improve patient compliance and diminish the prevalence of MDR resistance.


2010 ◽  
Vol 20 (9) ◽  
pp. 763-774 ◽  
Author(s):  
Stephan G. Maas ◽  
Gerhard Schaldach ◽  
Peter E. Walzel ◽  
Nora Anne Urbanetz

2012 ◽  
Vol 423 (2) ◽  
pp. 577-585 ◽  
Author(s):  
N. Mohajel ◽  
A. Roholamini Najafabadi ◽  
K. Azadmanesh ◽  
A. Vatanara ◽  
E. Moazeni ◽  
...  

2020 ◽  
Vol 23 (1) ◽  
Author(s):  
Maria F. Acosta ◽  
Michael D. Abrahamson ◽  
David Encinas-Basurto ◽  
Jeffrey R. Fineman ◽  
Stephen M. Black ◽  
...  

AbstractMetformin is an activator of the AMPK and Nrf2 pathways which are important in the pathology of several complex pulmonary diseases with unmet medical needs. Organic solution advanced spray drying in the absence of water in closed-mode was used to design and develop respirable dry powders. Following comprehensive characterization, the influence of physicochemical properties was correlated with performance as aerosols using inertial impaction and three different human dry powder inhaler (DPI) devices varying in device properties. In vitro cell assays were conducted to test safety in 2D human pulmonary cell lines and in 3D small airway epithelia comprising primary cells at the air-liquid interface (ALI). In addition, in vitro transepithelial electrical resistance (TEER) was carried out. Metformin remained crystalline following advanced spray drying under these conditions. All SD powders consisted of nanoparticles/microparticles in the solid state. In vitro aerosol dispersion performance showed high aerosolization for all SD metformin powders with all DPI devices tested. High emitted dose for all powders with all three DPI devices was measured. Differences in other aerosol performance parameters and the interplay between the properties of different formulations produced at specific pump rates and the three different DPI devices were correlated with spray drying pump rate and device properties. Safety over a wide metformin dose range was also demonstrated in vitro. Aerosol delivery of metformin nanoparticles/microparticles has the potential to be a new “first-in-class” therapeutic for the treatment of a number of pulmonary diseases including pulmonary vascular diseases such as pulmonary hypertension.


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