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Dry powder inhaler

Ziyu Zhao, Zhengwei Huang, Xuejuan Zhang, Ying Huang, Yingtong Cui, Cheng Ma, Guanlin Wang, Tim Freeman, Xiang-Yun Lu, Xin Pan, Chuanbin Wu
BACKGROUND: The hygroscopicity of raffinose carrier for dry powder inhaler (DPI) was the main obstacle for its further application. Hygroscopicity-induced agglomeration would cause deterioration of aerosolization performance of raffinose, undermining the delivery efficiency. METHODS: Cyclodextrin-raffinose binary carriers (CRBCs) were produced by spray-drying so as to surmount the above issue. Physicochemical attributes and formation mechanism of CRBCs were explored in detail...
March 13, 2018: Expert Opinion on Drug Delivery
Basanth Babu Eedara, Bhamini Rangnekar, Colin Doyle, Alex Cavallaro, Shyamal C Das
Pharmacotherapy of tuberculosis is potentially more efficient when delivered by the inhaled route than by the current oral and/or parenteral routes due to the higher concentration of drug reaching the primary region of infection in the lungs. This study investigated the influence of the amino acid L-leucine alone and in combination with the phospholipid, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), on the aerosolization behaviour of the anti-TB drugs, pyrazinamide and moxifloxacin HCl. Spray dried powders of pyrazinamide (P), moxifloxacin (M) alone and in combination with 10% L-leucine (PL and ML) and 10% DPPC (PLD and MLD) were produced...
March 7, 2018: International Journal of Pharmaceutics
Hyo-Jung Lee, Hong-Goo Lee, Yong-Bin Kwon, Ju-Young Kim, Yun-Seok Rhee, Jinmann Chon, Eun-Soek Park, Dong-Wook Kim, Chun-Woong Park
In this study, we prepared carrier-based formulations for dry powder inhalers by mixing bosentan microparticles with carrier, prepared in three separate types of lactose. Spray-dried, milled and sieved lactose resulted in formulations with various shapes, surface morphology and particle size distributions. In the spray-dried lactose, the micronized bosentan particles were trapped and strongly interlocked in the rugged surface of spray-dried lactose, whereas in the milled and sieved lactose they exhibited lower binding affinity onto the smooth surface of carrier...
March 3, 2018: European Journal of Pharmaceutical Sciences
Richard S Roberts, Sara Sevilla, Manel Ferrer, Joan Taltavull, Begoña Hernández, Victor Segarra, Jordi Gracia, Martin D Lehner, Amadeu Gavaldà, Míriam Andrés, Judit Cabedo, Dolors Vilella, Peter Eichhorn, Elena Calama, Carla Carcasona, Montserrat Miralpeix
Rational design of a novel template of naphthyridinones rapidly led to PDE4 inhibitors with sub-nanomolar enzymatic potencies. X-ray crystallography confirmed the binding mode of this novel template. We achieved compounds with double-digit picomolar enzymatic potencies through further structure-based design by targeting both the PDE4 enzyme metal-binding pocket and occupying the solvent-filled pocket. A strategy for lung retention and long duration of action based on low aqueous solubility was followed. In vivo efficacies were measured in a rat lung neutrophilia model by suspension microspray and dry powder administration...
March 5, 2018: Journal of Medicinal Chemistry
Birendra Chaurasiya, Liping Huang, Yunai Du, Baoqiang Tang, Zijie Qiu, Li Zhou, Jiasheng Tu, Chunmeng Sun
In this study, we prepared paclitaxel (PTX) loaded bovine serum albumin (BSA) microparticles (MPs) of different sizes (0.5, 1.0, and 3.0 µm) and converted them into dry powders (DPs) of a uniform size (∼5.0 µm) through spray-drying techniques. The aim of preparing different sized PTX-MPs is to investigate the size-based in vivo biodistribution and retention of PTX in the lungs after intratracheal administration. Following the in vitro characterizations, the anti-tumor efficacy of the DPs containing differently sized PTX-BSA-MPs administered through intratracheal insufflation was compared with intravenously administered PTX solution (Taxol)...
February 26, 2018: International Journal of Pharmaceutics
Kamaldeep Paul, Nitin Tandon, Runjhun Tandon, Harmanjit Singh Dosanjh, Vijay Luxami
Diabetes is a serious and chronic problem that can be attributed to the insufficient release of the insulin or when body does not respond to the insulin which is already present. This disease has been targeted for corrective action and implementation among four non-communicable diseases by world leaders according to WHO report. The prevalence of diabetes has been estimated to be double from 4.7% of adult population in 1980 to 8.5% in the present scenario. The estimated deaths due to this epidemic disease were 1...
February 28, 2018: Current Drug Delivery
Merja Kirjavainen, Leena Mattila, Mikko Vahteristo, Jani Korhonen, Satu Lähelmä
BACKGROUND: Easyhaler® dry powder inhaler (DPI) containing salmeterol and fluticasone propionate was developed for the treatment of asthma and chronic obstructive pulmonary disease. Three different Salmeterol/fluticasone Easyhaler test products (Orion Pharma, Finland) were compared against the reference product Seretide® Diskus® DPI (GlaxoSmithKline, United Kingdom) to study whether any of the test products are bioequivalent with the reference. METHODS: Open and randomized pharmacokinetic four-period crossover study on 65 healthy volunteers was performed in a single center to compare the lung deposition and total systemic exposure of salmeterol and fluticasone propionate after administration of single doses (two inhalations of 50/500 μg/inhalation strength) in fasting conditions...
March 1, 2018: Journal of Aerosol Medicine and Pulmonary Drug Delivery
Andrzej Emeryk, M Pirożyński, J Emeryk-Maksymiuk
The article briefly presents currently accessible dry powder inhalers (DPI). Basing on the data from the literature, we discussed the most common mistakes related to the utilisation of DPI as well as their clinical and economic consequences. We also extensively analysed all factors that may influence the efficacy and safety of inhaler therapy of asthma and COPD, mostly with the use of DPI. In addition, we indicated the potential to improve the efficacy of inhaler therapy from the doctor and COPD or asthma patient perspective...
2018: Advances in Respiratory Medicine
Bernice Mei Jin Tan, Lai Wah Chan, Paul Wan Sia Heng
Surface roughness is well recognized as a critical physical property of particulate systems, particularly in relation to adhesion, friction and flow. An example is the surface property of carrier particles in carrier-based dry powder inhaler (DPI) formulations. The numerical characterization of roughness remains rather unsatisfactory due to the lack of spatial (or length scale) information about surface features when a common amplitude parameter such as average roughness (Ra ) is used. An analysis of the roughness of lactose carrier particles at three different length scales, designed for specificity to the study of interactive mixtures in DPI, was explored in this study...
February 28, 2018: Molecular Pharmaceutics
A J Lexmond, S Keir, W Terakosolphan, C P Page, B Forbes
Inhaled adenosine receptor agonists induce bronchoconstriction and inflammation in asthma and are used as bronchial challenge agents for the diagnosis of asthma and in respiratory drug development. Recently developed dry powder aerosols of adenosine have several advantages over nebulised adenosine 5'-monophosphate (AMP) as bronchial challenge agents. However, reverse translation of this bronchial challenge technique to pre-clinical drug development is limited by the difficulty of administering powder aerosols to animals...
February 21, 2018: Drug Delivery and Translational Research
Daiki Hira, Hiroyoshi Koide, Shigemi Nakamura, Toyoko Okada, Kazunori Ishizeki, Masafumi Yamaguchi, Setsuko Koshiyama, Tetsuya Oguma, Kayoko Ito, Saori Funayama, Yuko Komase, Shin-Ya Morita, Kohshi Nishiguchi, Yasutaka Nakano, Tomohiro Terada
The patients' inhalation flow pattern is one of the significant determinants for clinical performance of inhalation therapy. However, the development of inhalation flow meters for various inhalation devices has been unable to keep up with the increasing number of newly launched inhalation devices. In the present study, we developed simple attachment orifices for the inhalation flow pattern monitoring system, which are suitable for all commercial inhalers, and investigated the efficacy of the system on the clinical inhalation instruction for patients co-prescribed dry powder inhaler (DPI) and soft mist inhaler (SMI)...
2018: PloS One
Mohammad A M Momin, Ian G Tucker, Colin S Doyle, John A Denman, Shubhra Sinha, Shyamal C Das
High dose delivery of drugs to the lung using a dry powder inhaler (DPI) is an emerging approach to combat drug-resistant local infections. To achieve this, highly aerosolizable powders are required. We hypothesized that co-spray-drying kanamycin, a hydrophilic hygroscopic antibiotic, with rifampicin, a hydrophobic antibiotic, would produce inhalable particles with surfaces enriched in rifampicin. Such particles would have higher aerosolization than kanamycin alone, and minimise the mass of powder for inhalation avoiding use of non-active excipients...
February 16, 2018: International Journal of Pharmaceutics
Ines Tomašek, Claire J Horwell, Christoph Bisig, David E Damby, Pierre Comte, Jan Czerwinski, Alke Petri-Fink, Martin J D Clift, Barbara Drasler, Barbara Rothen-Rutishauser
Communities resident in urban areas located near active volcanoes can experience volcanic ash exposures during, and following, an eruption, in addition to sustained exposures to high concentrations of anthropogenic air pollutants (e.g., vehicle exhaust emissions). Inhalation of anthropogenic pollution is known to cause the onset of, or exacerbate, respiratory and cardiovascular diseases. It is further postulated similar exposure to volcanic ash can also affect such disease states. Understanding of the impact of combined exposure of volcanic ash and anthropogenic pollution to human health, however, remains limited...
February 15, 2018: Environmental Pollution
Rawda Yaseen AlSheyyab, Bashar Mohammad Al-Taani, Rana Mohammad Obeidat, Motasem Mohammad Alsmadi, Rafeef Khalid Masaedeh, Raghda Nasry Sabat
GnRH antagonists have several clinical applications in prostate cancer, regulation of ovulation induction in females, breast cancer, male contraception and others. Antagonists differ from natural GnRH decapeptide in having five or more amino acid substitutions. Whereas most of antagonists are available as subcutaneous (SC) formula for injection, some are formulated as a depot formulation for sustained release (e.g. Cetrarelix, Degarelix). Systemic delivery of cetrorelix acetate by intratracheal route can be achieved using dry powder for inhalation of adhesive mixture when the powder deposition reaches stage four...
February 14, 2018: Current Drug Delivery
Jan Schulze, Stephanie Kuhn, Stephan Hendrikx, Michaela Schulz-Siegmund, Tobias Polte, Achim Aigner
Nucleic acid-based therapies rely on efficient formulations for nucleic acid protection and delivery. As nonviral strategies, polymeric and lipid-based nanoparticles have been introduced; however, biological efficacy and biocompatibility as well as poor storage properties due to colloidal instability and their unavailability as ready-to-use systems are still major issues. Polyethylenimine is the most widely explored and promising candidate for gene delivery. Polyethylenimine-based polyplexes and their combination with liposomes, lipopolyplexes, are efficient for DNA or siRNA delivery in vitro and in vivo...
February 12, 2018: Small
Daiki Hira, Tomoyuki Okuda, Ayano Mizutani, Nao Tomida, Hirokazu Okamoto
This study is aimed at developing a novel analytical method to identify optimal inhalation flow patterns for commercial dry powder inhalers (DPIs) and pressurized metered dose inhalers (pMDIs). As typical commercial DPI and pMDI, Pulmicort® Turbuhaler® and Sultanol® Inhaler were evaluated by an in-vitro inhalation performance testing system with a flow pattern simulator. An 8-stage Andersen cascade impactor (ACI) or twin stage liquid impinger (TSLI) was applied to determine the inhalation performance. The peak flow rate (PFR) of the inhalation flow pattern was set from 15 to 80 L/min in reference to our previous study...
February 8, 2018: Journal of Pharmaceutical Sciences
Alejandro Nieto-Orellana, David Coghlan, Malcolm Rothery, Franco H Falcone, Cynthia Bosquillon, Nick Childerhouse, Giuseppe Mantovani, Snow Stolnik
Pulmonary delivery of protein therapeutics has considerable clinical potential for treating both local and systemic diseases. However, poor protein conformational stability, immunogenicity and protein degradation by proteolytic enzymes in the lung are major challenges to overcome for the development of effective therapeutics. To address these, a family of structurally related copolymers comprising polyethylene glycol, mPEG2k, and poly(glutamic acid) with linear A-B (mPEG2k-lin-GA) and miktoarm A-B3 (mPEG2k-mik-(GA)3) macromolecular architectures was investigated as potential protein stabilisers...
February 6, 2018: International Journal of Pharmaceutics
Sarah J Nevitt, Judith Thornton, Clare S Murray, Tiffany Dwyer
BACKGROUND: Several agents are used to clear secretions from the airways of people with cystic fibrosis. Mannitol increases mucociliary clearance, but its exact mechanism of action is unknown. The dry powder formulation of mannitol may be more convenient and easier to use compared with established agents which require delivery via a nebuliser. Phase III trials of inhaled dry powder mannitol for the treatment of cystic fibrosis have been completed and it is now available in Australia and some countries in Europe...
February 9, 2018: Cochrane Database of Systematic Reviews
Thomas L Jones, Daniel M Neville, Anoop J Chauhan
Asthma and chronic obstructive pulmonary disease are primarily treated with inhaled medication, but delivery of that medication to its site of action is problematic; patients' ability to use inhalers will affect therapeutic response. Multiple inhaler devices are available but they are variably easy to use with consequent effects on compliance, intentional or otherwise. The Ellipta® device is a novel blister strip dry powder inhaler with medium resistance and a consistent delivered dose across a range of inspiratory flow rates...
February 1, 2018: Therapeutic Delivery
Liqun Wang, Ruirui Zhou, Xiaohui Xie
OBJECTIVE: To assess the efficacy and safety profile of tiotropium when added to low- to medium-dose inhaled corticosteroid (ICS) regimen versus low- to medium-dose ICS alone for adults with mild to moderate uncontrolled persistent asthma. DATA SOURCES: The online databases Pubmed, Embase and the Cochrane Library were searched for relevant data published up to November 14, 2017; we also conducted a supplementary search using STUDY SELECTIONS: Only randomized control trials were included in this review...
February 8, 2018: Journal of Asthma: Official Journal of the Association for the Care of Asthma
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