scholarly journals Excipient Interactions in Glucagon Dry Powder Inhaler Formulation for Pulmonary Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 207 ◽  
Author(s):  
Md Abdur Rashid ◽  
Amged Awad Elgied ◽  
Yahya Alhamhoom ◽  
Enoch Chan ◽  
Llew Rintoul ◽  
...  
Keyword(s):  
Dry Powder Inhaler ◽  
Pulmonary Delivery ◽  
Magnesium Stearate ◽  
Dry Powder ◽  
Scanning Calorimetry ◽  
Physical Interactions ◽  
A Minor ◽  
Excipient Interactions ◽  
Glucagon Concentration

Purpose: This study describes the development and characterization of glucagon dry powder inhaler (DPI) formulation for pulmonary delivery. Lactose monohydrate, as a carrier, and L-leucine and magnesium stearate (MgSt) were used as dispersibility enhancers for this formulation. Methods: Using Fourier-transform infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), and Raman confocal microscopy, the interactions between glucagon and all excipients were characterized. The fine particle fractions (FPFs) of glucagon in different formulations were determined by a twin stage impinger (TSI) using a 2.5% glucagon mixture, and the glucagon concentration was measured by a validated LC-MS/MS method. Results: The FPF of the glucagon was 6.4%, which increased six-fold from the formulations with excipients. The highest FPF (36%) was observed for the formulation containing MgSt and large carrier lactose. The FTIR, Raman, and DSC data showed remarkable physical interactions of glucagon with leucine and a minor interaction with lactose; however, there were no interactions with MgSt alone or mixed with lactose. Conclusion: Due to the interaction between L-leucine and glucagon, leucine was not a suitable excipient for glucagon formulation. In contrast, the use of lactose and MgSt could be considered to prepare an efficient DPI formulation for the pulmonary delivery of glucagon.

scholarly journals Puerarin dry powder inhaler formulations for pulmonary delivery: Development and characterization

PLoS ONE ◽  
2021 ◽  
Vol 16 (4) ◽  
pp. e0249683
Author(s):  
Md Abdur Rashid ◽  
Saiqa Muneer ◽  
Tony Wang ◽  
Yahya Alhamhoom ◽  
Llew Rintoul ◽  
...  
Keyword(s):  
Low Dose ◽  
Structural Integrity ◽  
Dry Powder Inhaler ◽  
Pulmonary Delivery ◽  
Magnesium Stearate ◽  
Hplc Method ◽  
Dry Powder ◽  
Scanning Calorimetry ◽  
X Ray

This study aims at developing and characterizing the puerarin dry powder inhaler (DPI) formulations for pulmonary delivery. The inhalable particles size (<2 μm) was accomplished by micronization and its morphology was examined by scanning electron microscopy (SEM). The puerarin-excipient interaction in powder mixtures was analyzed by using Fourier transform infrared spectroscopy (FTIR), Raman confocal microscopy, X-Ray powder Diffraction (XRD), and differential scanning calorimetry (DSC) methods. Using a Twin stage impinger (TSI), the in-vitro aerosolization of the powder formulations was carried out at a flow rate of 60 L/min and the drug was quantified by employing a validated HPLC method. No significant interactions between the drug and the excipients were observed in the powder formulations. The fine particle fraction (FPF) of the drug alone was 4.2% which has increased five to six-fold for the formulations with aerosolization enhancers. Formulation containing lactose as large carriers produced 32.7% FPF, which further increased with the addition of dispersibility enhancers, leucine and magnesium stearate (40.8% and 41.2%, respectively). The Raman and FTIR techniques are very useful tool for understanding structural integrity and stability of the puerarin in the powder formulations. The puerarin was found to be compatible with the excipients used and the developed DPI formulation may be considered as an efficient formulation for pulmonary delivery for the management of various diseases at a very low dose.

scholarly journals Preparation and Characterization of a Dry Powder Inhaler Composed of PLGA Large Porous Particles Encapsulating Gentamicin Sulfate

2019 ◽  
Vol 9 (2) ◽  
pp. 255-261 ◽  
Author(s):  
Farideh Shiehzadeh ◽  
Mohsen Tafaghodi ◽  
Majid Laal-Dehghani ◽  
Faezeh Mashhoori ◽  
Bibi Sedigheh Fazly Bazzaz ◽  
...  
Keyword(s):  
Dry Powder Inhaler ◽  
Pulmonary Delivery ◽  
Dry Powder ◽  
Scanning Calorimetry ◽  
Porous Particles ◽  
Gentamicin Sulfate ◽  
Freeze Dried ◽  
Emulsification Solvent Evaporation

Purpose: Direct delivery of aminoglycosides to the lungs was under extensive evaluations during the last decades. Because of large particle size, low density and porous structure, large porous particles (LPPs) are versatile carriers for this purpose. In this study, poly (lactic-co-glycolic acid) (PLGA) LPPs encapsulating gentamicin sulfate were prepared and in vitro characteristics of their freeze-dried powder as a dry powder inhaler (DPI) were evaluated. Methods: To prepare PLGA LPPs, a double emulsification-solvent evaporation method was optimized and gentamicin sulfate was post-loaded in the LPPs. In vitro characteristics including morphological features, thermal behavior, aerodynamic profile and cumulative drug release were evaluated by the scanning electron microscope (SEM), differential scanning calorimetry (DSC), next-generation cascade impactor (NGI) and Franz diffusion cell respectively. Results: The obtained results revealed that the preparation method was capable to produce spherical large homogenous highly porous particles. 94% of gentamicin sulfate released from LPPs up to 30 minutes. Mass median aerodynamic diameter (MMAD) and fine particle fraction (FPF) were 4.9 µm and 39% respectively. Conclusion: In this study, dry powder formulation composed of PLGA LPPs encapsulating gentamicin sulfate showed a promising in vitro behavior as a pulmonary delivery carrier. Improvements on the aerodynamic behavior and in vivo evaluations recommended for further developments.

scholarly journals Development of a Carrier Free Dry Powder Inhalation Formulation of Ketotifen for Pulmonary Drug Delivery

Drug Research ◽  
2019 ◽  
Vol 70 (01) ◽  
pp. 26-32
Author(s):  
Fariba Azari ◽  
Saeed Ghanbarzadeh ◽  
Rezvan Safdari ◽  
Shadi Yaqoubi ◽  
Khosro Adibkia ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Spray Drying ◽  
Dry Powder Inhaler ◽  
Ammonium Bicarbonate ◽  
Pulmonary Drug Delivery ◽  
Water Mixture ◽  
Dry Powder ◽  
Scanning Calorimetry ◽  
Aerodynamic Properties ◽  
Systemic Treatments

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.

Novel dry powder inhaler formulation of glucagon with addition of citric acid for enhanced pulmonary delivery

2009 ◽  
Vol 382 (1-2) ◽  
pp. 144-150 ◽  
Author(s):  
Satomi Onoue ◽  
Kiyoshi Yamamoto ◽  
Yohei Kawabata ◽  
Mariko Hirose ◽  
Takahiro Mizumoto ◽  
...  
Keyword(s):  
Citric Acid ◽  
Dry Powder Inhaler ◽  
Pulmonary Delivery ◽  
Dry Powder

scholarly journals Design and Comprehensive Characterization of Tetramethylpyrazine (TMP) for Targeted Lung Delivery as Inhalation Aerosols in Pulmonary Hypertension (PH): In Vitro Human Lung Cell Culture and In Vivo Efficacy

Antioxidants ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 427
Author(s):  
Priya Muralidharan ◽  
Maria F. Acosta ◽  
Alexan I. Gomez ◽  
Carissa Grijalva ◽  
Haiyang Tang ◽  
...  
Keyword(s):  
Human Lung ◽  
Antioxidant Properties ◽  
Dry Powder Inhaler ◽  
Chinese Herbs ◽  
Dry Powder ◽  
Comprehensive Characterization ◽  
Spray Dried

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.

scholarly journals Inhaled ciprofloxacin-loaded poly(2-ethyl-2-oxazoline) nanoparticles from dry powder inhaler formulation for the potential treatment of lower respiratory tract infections

PLoS ONE ◽  
2021 ◽  
Vol 16 (12) ◽  
pp. e0261720
Author(s):  
Mohammad Zaidur Rahman Sabuj ◽  
Tim R. Dargaville ◽  
Lisa Nissen ◽  
Nazrul Islam
Keyword(s):  
Respiratory Tract ◽  
Lower Respiratory Tract ◽  
Respiratory Tract Infections ◽  
Drug Loading ◽  
Dry Powder Inhaler ◽  
Pulmonary Delivery ◽  
Lower Respiratory Tract Infections ◽  
Dry Powder ◽  
Tract Infections

Lower respiratory tract infections (LRTIs) are one of the fatal diseases of the lungs that have severe impacts on public health and the global economy. The currently available antibiotics administered orally for the treatment of LRTIs need high doses with frequent administration and cause dose-related adverse effects. To overcome this problem, we investigated the development of ciprofloxacin (CIP) loaded poly(2-ethyl-2-oxazoline) (PEtOx) nanoparticles (NPs) for potential pulmonary delivery from dry powder inhaler (DPI) formulations against LRTIs. NPs were prepared using a straightforward co-assembly reaction carried out by the intermolecular hydrogen bonding among PEtOx, tannic acid (TA), and CIP. The prepared NPs were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction analysis (PXRD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). The CIP was determined by validated HPLC and UV spectrophotometry methods. The CIP loading into the PEtOx was between 21–67% and increased loading was observed with the increasing concentration of CIP. The NP sizes of PEtOx with or without drug loading were between 196–350 nm and increased with increasing drug loading. The in vitro CIP release showed the maximum cumulative release of about 78% in 168 h with a burst release of 50% in the first 12 h. The kinetics of CIP release from NPs followed non-Fickian or anomalous transport thus suggesting the drug release was regulated by both diffusion and polymer degradation. The in vitro aerosolization study carried out using a Twin Stage Impinger (TSI) at 60 L/min air flow showed the fine particle fraction (FPF) between 34.4% and 40.8%. The FPF was increased with increased drug loading. The outcome of this study revealed the potential of the polymer PEtOx as a carrier for developing CIP-loaded PEtOx NPs as DPI formulation for pulmonary delivery against LRTIs.

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