The Experts below are selected from a list of 2559 Experts worldwide ranked by ideXlab platform
Rita Ambrus - One of the best experts on this subject based on the ideXlab platform.
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development of an innovative carrier based dry powder Inhalation Formulation containing spray dried meloxicam potassium to improve the in vitro and in silico aerodynamic properties
Pharmaceutics, 2020Co-Authors: Edit Benke, Piroska Szaborevesz, Arpad Farkas, Rita AmbrusAbstract:Most of the marketed dry powder Inhalation (DPI) products are traditional, carrier-based Formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new Formulation, confirming that the interparticle interactions were changed favorably.
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development of a microparticle based dry powder Inhalation Formulation of ciprofloxacin hydrochloride applying the quality by design approach
Drug Design Development and Therapy, 2016Co-Authors: Keyhaneh Karimi, Edina Pallagi, Piroska Szaborevesz, Ildiko Csoka, Rita AmbrusAbstract:Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder Inhalation Formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder Formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These Formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%.
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new aspects of developing a dry powder Inhalation Formulation applying the quality by design approach
International Journal of Pharmaceutics, 2016Co-Authors: Edina Pallagi, Keyhaneh Karimi, Rita Ambrus, Piroska Szaborevesz, Ildiko CsokaAbstract:Abstract The current work outlines the application of an up-to-date and regulatory-based pharmaceutical quality management method, applied as a new development concept in the process of formulating dry powder Inhalation systems (DPIs). According to the Quality by Design (QbD) methodology and Risk Assessment (RA) thinking, a mannitol based co-spray dried formula was produced as a model dosage form with meloxicam as the model active agent. The concept and the elements of the QbD approach (regarding its systemic, scientific, risk-based, holistic, and proactive nature with defined steps for pharmaceutical development), as well as the experimental drug Formulation (including the technological parameters assessed and the methods and processes applied) are described in the current paper. Findings of the QbD based theoretical prediction and the results of the experimental development are compared and presented. Characteristics of the developed end-product were in correlation with the predictions, and all data were confirmed by the relevant results of the in vitro investigations. These results support the importance of using the QbD approach in new drug Formulation, and prove its good usability in the early development process of DPIs. This innovative Formulation technology and product appear to have a great potential in pulmonary drug delivery.
Hamed Hamishehkar - One of the best experts on this subject based on the ideXlab platform.
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co electrospraying technology as a novel approach for dry powder Inhalation Formulation of montelukast and budesonide for pulmonary co delivery
International Journal of Pharmaceutics, 2020Co-Authors: Shadi Yaqoubi, Khosro Adibkia, Hamed Hamishehkar, Ali Nokhodchi, Shahram Emami, Ali Akbar Alizadeh, Mohammad BarzegarjalaliAbstract:In the current study electrospraying methodology was used for particle engineering of montelukast and budesonide to prepare a combined inhalable dry powder Formulation applicable as a smart regimen in asthma treatment. For this, electrospraying was carried out using different solvents and drug concentrations. No carrier was added for the Formulation of montelukast-budesonide combination as montelukast played the role of both active ingredient and carrier. Scanning electron microscopy, particle size analysis, gas chromatography, powder X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were used to evaluate the physicochemical properties of the produced drug particles. In vitro drug deposition pattern was assessed using next generation impactor, and the dissolution profile of the selected Formulations was characterized via modified diffusion franz cell method. The FPF value for the co-electrosprayed carrier free Formulation of montelukast-budesonide was 38% with a significantly enhanced dissolution rate for budesonide compared to the budesonide alone Formulations. The pharmacological effects of hypothesized combined Formulation was assessed by measuring its power to inhibit the production of reactive oxygen species in human normal lung cells. The results showed that the combination of montelukast and budesonide can exert a synergistic effect. The findings in the current study emphasize that using montelukast as a carrier for budesonide not only has greatly improved the aerosolization behavior and dissolution rate of budesonide but also has resulted in synergistic pharmacological effects, indicating the suitability of this combination as an anti-asthmatic therapeutic.
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development of a carrier free dry powder Inhalation Formulation of ketotifen for pulmonary drug delivery
Drug Research, 2020Co-Authors: Fariba Azari, Saeed Ghanbarzadeh, Khosro Adibkia, Rezvan Safdari, Shadi Yaqoubi, Hamed HamishehkarAbstract: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.
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a multilayer hollow nanocarrier for pulmonary co drug delivery of methotrexate and doxorubicin in the form of dry powder Inhalation Formulation
Materials Science and Engineering: C, 2019Co-Authors: Saeideh Nozohouri, Roya Salehi, Saeed Ghanbarzadeh, Khosro Adibkia, Hamed HamishehkarAbstract:Lung cancer is the number one cause of cancer deaths in the global population and remains difficult to treat mainly because of the absence of targeted drug delivery stages and restrictions related with delivery of drugs to deep lung tissues. The aim of the present study was to develop a noninvasive, patient-convenient Formulation for the targeted delivery of chemotherapeutics to cancer cells located in the deep lung tissue. A PEGylated paramagnetic hollow-nanosphere was fabricated, fully characterized and used as a nanocarrier for pulmonary co-delivery of Doxorubicin (DOX) and Methotrexate (MTX). In first step, magnetic-silica nanoparticles were synthesized and then coated with amino/acrylate groups and derivatized with polyethylene glycol (PEG). Finally, silica was removed to provide hollow structured nanoparticles. The biocompatibility of blank carriers and the efficiency of MTX-DOX-loaded carriers were also approved by MTT assay and DAPI staining. The aerosolization performance of nanoparticles embedded microspheres were assessed by next generation impactor. The almost natural zeta potential and obvious decrease in silica content observed by EDX and removal of intense silica characteristic peak at FTIR analyses approved the successful removal of silica layer and preparation of hollow-nanospheres. The successful PEGylation of multilayer magnetic hollow-nanospheres catalyzed by boric acid was confirmed by presence of amide groups in FTIR spectra. The developed polymeric nanoparticle showed quite appropriate loading capacity for both DOX and MTX (48%) because of designing adequate negatively and positively charged sites for both drugs. The cytotoxicity assays proved the safety of blank nanoparticles and efficacy of drugs-loaded nanoparticles on lung cancer A549 cell lines. The developed dry powder Inhalation Formulation of nanoparticles showed appropriate aerosolization performance (fine particle fraction around 22%). It was concluded that these outcomes may open the potentials for efficient pulmonary co-delivery of MTX and DOX to the carcinogenic tissues.
Keyhaneh Karimi - One of the best experts on this subject based on the ideXlab platform.
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development of a microparticle based dry powder Inhalation Formulation of ciprofloxacin hydrochloride applying the quality by design approach
Drug Design Development and Therapy, 2016Co-Authors: Keyhaneh Karimi, Edina Pallagi, Piroska Szaborevesz, Ildiko Csoka, Rita AmbrusAbstract:Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder Inhalation Formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder Formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These Formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%.
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new aspects of developing a dry powder Inhalation Formulation applying the quality by design approach
International Journal of Pharmaceutics, 2016Co-Authors: Edina Pallagi, Keyhaneh Karimi, Rita Ambrus, Piroska Szaborevesz, Ildiko CsokaAbstract:Abstract The current work outlines the application of an up-to-date and regulatory-based pharmaceutical quality management method, applied as a new development concept in the process of formulating dry powder Inhalation systems (DPIs). According to the Quality by Design (QbD) methodology and Risk Assessment (RA) thinking, a mannitol based co-spray dried formula was produced as a model dosage form with meloxicam as the model active agent. The concept and the elements of the QbD approach (regarding its systemic, scientific, risk-based, holistic, and proactive nature with defined steps for pharmaceutical development), as well as the experimental drug Formulation (including the technological parameters assessed and the methods and processes applied) are described in the current paper. Findings of the QbD based theoretical prediction and the results of the experimental development are compared and presented. Characteristics of the developed end-product were in correlation with the predictions, and all data were confirmed by the relevant results of the in vitro investigations. These results support the importance of using the QbD approach in new drug Formulation, and prove its good usability in the early development process of DPIs. This innovative Formulation technology and product appear to have a great potential in pulmonary drug delivery.
Piroska Szaborevesz - One of the best experts on this subject based on the ideXlab platform.
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development of an innovative carrier based dry powder Inhalation Formulation containing spray dried meloxicam potassium to improve the in vitro and in silico aerodynamic properties
Pharmaceutics, 2020Co-Authors: Edit Benke, Piroska Szaborevesz, Arpad Farkas, Rita AmbrusAbstract:Most of the marketed dry powder Inhalation (DPI) products are traditional, carrier-based Formulations with low drug concentrations deposited in the lung. However, due to their advantageous properties, their development has become justified. In our present work, we developed an innovative, carrier-based DPI system, which is an interactive physical blend of a surface-modified carrier and a spray-dried drug with suitable shape and size for pulmonary application. Meloxicam potassium, a nonsteroidal anti-inflammatory drug (NSAID), was used as an active ingredient due to its local anti-inflammatory effect and ability to decrease the progression of cystic fibrosis (CF) and chronic obstructive pulmonary disease (COPD). The results of the in vitro and in silico investigations showed high lung deposition in the case of this new Formulation, confirming that the interparticle interactions were changed favorably.
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development of a microparticle based dry powder Inhalation Formulation of ciprofloxacin hydrochloride applying the quality by design approach
Drug Design Development and Therapy, 2016Co-Authors: Keyhaneh Karimi, Edina Pallagi, Piroska Szaborevesz, Ildiko Csoka, Rita AmbrusAbstract:Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder Inhalation Formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder Formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These Formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%.
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new aspects of developing a dry powder Inhalation Formulation applying the quality by design approach
International Journal of Pharmaceutics, 2016Co-Authors: Edina Pallagi, Keyhaneh Karimi, Rita Ambrus, Piroska Szaborevesz, Ildiko CsokaAbstract:Abstract The current work outlines the application of an up-to-date and regulatory-based pharmaceutical quality management method, applied as a new development concept in the process of formulating dry powder Inhalation systems (DPIs). According to the Quality by Design (QbD) methodology and Risk Assessment (RA) thinking, a mannitol based co-spray dried formula was produced as a model dosage form with meloxicam as the model active agent. The concept and the elements of the QbD approach (regarding its systemic, scientific, risk-based, holistic, and proactive nature with defined steps for pharmaceutical development), as well as the experimental drug Formulation (including the technological parameters assessed and the methods and processes applied) are described in the current paper. Findings of the QbD based theoretical prediction and the results of the experimental development are compared and presented. Characteristics of the developed end-product were in correlation with the predictions, and all data were confirmed by the relevant results of the in vitro investigations. These results support the importance of using the QbD approach in new drug Formulation, and prove its good usability in the early development process of DPIs. This innovative Formulation technology and product appear to have a great potential in pulmonary drug delivery.
Khosro Adibkia - One of the best experts on this subject based on the ideXlab platform.
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co electrospraying technology as a novel approach for dry powder Inhalation Formulation of montelukast and budesonide for pulmonary co delivery
International Journal of Pharmaceutics, 2020Co-Authors: Shadi Yaqoubi, Khosro Adibkia, Hamed Hamishehkar, Ali Nokhodchi, Shahram Emami, Ali Akbar Alizadeh, Mohammad BarzegarjalaliAbstract:In the current study electrospraying methodology was used for particle engineering of montelukast and budesonide to prepare a combined inhalable dry powder Formulation applicable as a smart regimen in asthma treatment. For this, electrospraying was carried out using different solvents and drug concentrations. No carrier was added for the Formulation of montelukast-budesonide combination as montelukast played the role of both active ingredient and carrier. Scanning electron microscopy, particle size analysis, gas chromatography, powder X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were used to evaluate the physicochemical properties of the produced drug particles. In vitro drug deposition pattern was assessed using next generation impactor, and the dissolution profile of the selected Formulations was characterized via modified diffusion franz cell method. The FPF value for the co-electrosprayed carrier free Formulation of montelukast-budesonide was 38% with a significantly enhanced dissolution rate for budesonide compared to the budesonide alone Formulations. The pharmacological effects of hypothesized combined Formulation was assessed by measuring its power to inhibit the production of reactive oxygen species in human normal lung cells. The results showed that the combination of montelukast and budesonide can exert a synergistic effect. The findings in the current study emphasize that using montelukast as a carrier for budesonide not only has greatly improved the aerosolization behavior and dissolution rate of budesonide but also has resulted in synergistic pharmacological effects, indicating the suitability of this combination as an anti-asthmatic therapeutic.
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development of a carrier free dry powder Inhalation Formulation of ketotifen for pulmonary drug delivery
Drug Research, 2020Co-Authors: Fariba Azari, Saeed Ghanbarzadeh, Khosro Adibkia, Rezvan Safdari, Shadi Yaqoubi, Hamed HamishehkarAbstract: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.
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a multilayer hollow nanocarrier for pulmonary co drug delivery of methotrexate and doxorubicin in the form of dry powder Inhalation Formulation
Materials Science and Engineering: C, 2019Co-Authors: Saeideh Nozohouri, Roya Salehi, Saeed Ghanbarzadeh, Khosro Adibkia, Hamed HamishehkarAbstract:Lung cancer is the number one cause of cancer deaths in the global population and remains difficult to treat mainly because of the absence of targeted drug delivery stages and restrictions related with delivery of drugs to deep lung tissues. The aim of the present study was to develop a noninvasive, patient-convenient Formulation for the targeted delivery of chemotherapeutics to cancer cells located in the deep lung tissue. A PEGylated paramagnetic hollow-nanosphere was fabricated, fully characterized and used as a nanocarrier for pulmonary co-delivery of Doxorubicin (DOX) and Methotrexate (MTX). In first step, magnetic-silica nanoparticles were synthesized and then coated with amino/acrylate groups and derivatized with polyethylene glycol (PEG). Finally, silica was removed to provide hollow structured nanoparticles. The biocompatibility of blank carriers and the efficiency of MTX-DOX-loaded carriers were also approved by MTT assay and DAPI staining. The aerosolization performance of nanoparticles embedded microspheres were assessed by next generation impactor. The almost natural zeta potential and obvious decrease in silica content observed by EDX and removal of intense silica characteristic peak at FTIR analyses approved the successful removal of silica layer and preparation of hollow-nanospheres. The successful PEGylation of multilayer magnetic hollow-nanospheres catalyzed by boric acid was confirmed by presence of amide groups in FTIR spectra. The developed polymeric nanoparticle showed quite appropriate loading capacity for both DOX and MTX (48%) because of designing adequate negatively and positively charged sites for both drugs. The cytotoxicity assays proved the safety of blank nanoparticles and efficacy of drugs-loaded nanoparticles on lung cancer A549 cell lines. The developed dry powder Inhalation Formulation of nanoparticles showed appropriate aerosolization performance (fine particle fraction around 22%). It was concluded that these outcomes may open the potentials for efficient pulmonary co-delivery of MTX and DOX to the carcinogenic tissues.