Development of a new formulation of roflumilast for pulmonary drug delivery to treat inflammatory lung conditions.
作者： Érika Yoko Suzuki , Maria Inês Amaro , Gabriella Silva de Almeida , Lucio Mendes Cabral , Anne Marie Healy
DOI: 10.1016/J.IJPHARM.2018.08.035
关键词: Particle size 、 Particle-size distribution 、 Roflumilast 、 Scanning electron microscope 、 Materials science 、 Chemical engineering 、 Specific surface area 、 Drug delivery 、 Particle 、 Spray drying
摘要: The aim of this study was to develop roflumilast dry powder inhaler (DPI) formulations by spray drying using hydroxypropyl-β-cyclodextrin (HPβCD) and determine their suitability for pulmonary delivery. Different feed solution concentrations, solvent systems parameters were used obtain the which characterized X-ray diffraction, thermal analysis, scanning electron microscopy, particle size distribution, bulk tapped density, specific surface area, dynamic vapour sorption, in vitro deposition properties a Next Generation Impactor (NGI) transepithelial permeability. Microparticles dried from ethanol wrinkled amorphous, exhibiting high glass transition temperatures while those methanol:n-butyl acetate consisted irregularly shaped porous particles partially crystalline. All presented low residual content depositon lower stages NGI. Mass median aerodynamic diameters (MMADs) range 3.32-4.49 μm, with fine fractions (FPF < 5 μm). Stability studies demonstrated no significant modifications solid-state nature aerolisation performance selected formulation Papp 8.73 × 10-6 ± 4.70 10-7 cm/s. developed DPI have potential therapeutic applications treatment lung diseases.
sci-hub.se 参考文章(45)
Alejandro Sosnik, Katia P. Seremeta, Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers Advances in Colloid and Interface Science. ,vol. 223, pp. 40- 54 ,(2015) , 10.1016/J.CIS.2015.05.003
Krzysztof J. Paluch, Lidia Tajber, Owen I. Corrigan, Anne Marie Healy, Impact of process variables on the micromeritic and physicochemical properties of spray-dried porous microparticles, part I: introduction of a new morphology classification system Journal of Pharmacy and Pharmacology. ,vol. 64, pp. 1570- 1582 ,(2012) , 10.1111/J.2042-7158.2012.01539.X
Gilles Dufour, William Bigazzi, Nelson Wong, Frederic Boschini, Pascal de Tullio, Geraldine Piel, Didier Cataldo, Brigitte Evrard, Interest of cyclodextrins in spray-dried microparticles formulation for sustained pulmonary delivery of budesonide. International Journal of Pharmaceutics. ,vol. 495, pp. 869- 878 ,(2015) , 10.1016/J.IJPHARM.2015.09.052
D Tabor, Surface forces and surface interactions Journal of Colloid and Interface Science. ,vol. 58, pp. 2- 13 ,(1977) , 10.1016/0021-9797(77)90366-6
A HEALY, B MCDONALD, L TAJBER, O CORRIGAN, Characterisation of excipient-free nanoporous microparticles (NPMPs) of bendroflumethiazide European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 69, pp. 1182- 1186 ,(2008) , 10.1016/J.EJPB.2008.04.020
Frederic Tewes, Carsten Ehrhardt, Anne Marie Healy, Superparamagnetic iron oxide nanoparticles (SPIONs)-loaded Trojan microparticles for targeted aerosol delivery to the lung European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 86, pp. 98- 104 ,(2014) , 10.1016/J.EJPB.2013.09.004
Maria Inês Amaro, Frederic Tewes, Oliviero Gobbo, Lidia Tajber, Owen I. Corrigan, Carsten Ehrhardt, Anne Marie Healy, Formulation, stability and pharmacokinetics of sugar-based salmon calcitonin-loaded nanoporous/nanoparticulate microparticles (NPMPs) for inhalation. International Journal of Pharmaceutics. ,vol. 483, pp. 6- 18 ,(2015) , 10.1016/J.IJPHARM.2015.02.003
K. S. W. Sing, Reporting physisorption data for gas/solid systems with special reference to the determination of surface area and porosity (Recommendations 1984) Pure and Applied Chemistry. ,vol. 57, pp. 603- 619 ,(1985) , 10.1351/PAC198557040603
Neil R. Mathias, Julita Timoszyk, Paul I. Stetsko, John R. Megill, Ronald L. Smith, Doris A. Wall, Permeability characteristics of calu-3 human bronchial epithelial cells: in vitro-in vivo correlation to predict lung absorption in rats. Journal of Drug Targeting. ,vol. 10, pp. 31- 40 ,(2002) , 10.1080/10611860290007504
Sidney John Gregg, Adsorption, Surface Area and Porosity ,(1967)