Development of Spray Dried Liposomal Dry Powder Inhaler of Dapsone

This is the first study reporting on the design and development innovative inhaled formulations of the novel natural product antioxidant therapeutic, tetramethylpyrazine (TMP), also known as ligustrazine. TMP is obtained from Chinese herbs belonging to the class of Ligusticum. It is known to have antioxidant properties. It can act as a Nrf2/ARE activator and a Rho/ROCK inhibitor. The present study reports for the first time on the comprehensive characterization of raw TMP (non-spray dried) and spray dried TMP in a systematic manner using thermal analysis, electron microscopy, optical microscopy, and Raman spectroscopy. The in vitro aerosol dispersion performance of spray dried TMP was tested using three different FDA-approved unit-dose capsule-based human dry powder inhaler devices. In vitro human cellular studies were conducted on pulmonary cells from different regions of the human lung to examine the biocompatibility and non-cytotoxicity of TMP. Furthermore, the efficacy of inhaled TMP as both liquid and dry powder inhalation aerosols was tested in vivo using the monocrotaline (MCT)-induced PH rat model.

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Dry powder inhaler performance of spray dried mannitol with tailored surface morphologies as carrier and salbutamol sulphate

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2017.03.055 ◽

2017 ◽

Vol 524 (1-2) ◽

pp. 351-363 ◽

Cited By ~ 10

Author(s):

M. Mönckedieck ◽

J. Kamplade ◽

P. Fakner ◽

N.A. Urbanetz ◽

P. Walzel ◽

...

Keyword(s):

Dry Powder Inhaler ◽

Dry Powder ◽

Salbutamol Sulphate ◽

Surface Morphologies ◽

Spray Dried ◽

Spray Dried Mannitol ◽

Inhaler Performance

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Towards a More Desirable Dry Powder Inhaler Formulation: Large Spray-Dried Mannitol Microspheres Outperform Small Microspheres

Pharmaceutical Research ◽

10.1007/s11095-013-1132-2 ◽

2013 ◽

Vol 31 (1) ◽

pp. 60-76 ◽

Cited By ~ 31

Author(s):

Waseem Kaialy ◽

Tariq Hussain ◽

Amjad Alhalaweh ◽

Ali Nokhodchi

Keyword(s):

Dry Powder Inhaler ◽

Dry Powder ◽

Spray Dried ◽

Spray Dried Mannitol

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Nano-Liposomal Dry Powder Inhaler of Amiloride Hydrochloride

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2006.405 ◽

2006 ◽

Vol 6 (9) ◽

pp. 3001-3009 ◽

Cited By ~ 23

Author(s):

Mahavir Bhupal Chougule ◽

Bijay Kumar Padhi ◽

Ambikanandan Misra

Keyword(s):

Cystic Fibrosis ◽

Drug Release ◽

Phosphate Buffer ◽

Dry Powder Inhaler ◽

Dry Powder ◽

Phosphate Buffer Saline ◽

Amiloride Hydrochloride ◽

Spray Dried

The purpose of this study was to encapsulate Amiloride Hydrochloride into nano-liposomes, incorporate it into dry powder inhaler, and to provide prolonged effective concentration in airways to enhance mucociliary clearance and prevent secondary infection in cystic fibrosis. Liposomes were prepared by thin film hydration technique and then dispersion was passed through high pressure homogenizer to achieve size of nanometer range. Nano-liposomes were separated by centrifugation and were characterized. They were dispersed in phosphate buffer saline pH 7.4 containing carriers (lactose/sucrose/mannitol), and glycine as anti-adherent. The resultant dispersion was spray dried. The spray dried powders were characterized and in vitro drug release studies were performed using phosphate buffer saline pH 7.4. in vitro and in vivo drug pulmonary deposition was carried out using Andersen Cascade Impactor and by estimating drug in bronchial alveolar lavage and lung homogenate after intratracheal instillation in rats respectively. Nano-liposomes were found to have mean volume diameter of 198 ± 15 nm, and 57% ± 1.9% of drug entrapment. Mannitol based formulation was found to have low density, good flowability, particle size of 6.7 ± 0.6 μm determined by Malvern MasterSizer, maximum fine particle fraction of 67.6 ± 0.6%, mean mass aerodynamic diameter 2.3 ± 0.1 μm, and geometric standard deviation 2.4 ± 0.1. Developed formulations were found to have prolonged drug release following Higuchi's Controlled Release model and in vivo studies showed maximal retention time of drug of 12 hrs within the lungs and slow clearance from the lungs. This study provides a practical approach for direct lung delivery of Amiloride Hydrochloride encapsulated in liposomes for controlled and prolonged retention at the site of action from dry powder inhaler. It can provide a promising alternative to the presently available nebulizers in terms of prolonged pharmacological effect, reducing systemic side effects such as potassium retention due to rapid clearance of the drug from lungs in patients suffering from cystic fibrosis.

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The Deposition of Spray-Dried p-Galactosidase from Dry Powder Inhaler Devices

Drug Development and Industrial Pharmacy ◽

10.3109/03639049609065911 ◽

1996 ◽

Vol 22 (8) ◽

pp. 813-822 ◽

Cited By ~ 13

Author(s):

J. Broadhead ◽

S. K. Edmond Rouan ◽

C. T. Rhodes

Keyword(s):

Dry Powder Inhaler ◽

Dry Powder ◽

Inhaler Devices ◽

Spray Dried

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

Pharmaceutics ◽

10.3390/pharmaceutics12080765 ◽

2020 ◽

Vol 12 (8) ◽

pp. 765

Author(s):

Yong-Bin Kwon ◽

Ji-Hyun Kang ◽

Chang-Soo Han ◽

Dong-Wook Kim ◽

Chun-Woong Park

Keyword(s):

Particle Size ◽

Smooth Surface ◽

Dry Powder Inhaler ◽

Aerodynamic Performance ◽

Dry Powder ◽

Andersen Cascade Impactor ◽

Scanning Calorimetry ◽

Spherical Morphology ◽

Aerodynamic Properties ◽

Spray Dried

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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