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Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols.
Drug Des Devel Ther. 2016; 10:4017-4030.DD

Abstract

The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa. The physicochemical properties of the spray-dried (SD) and jet-milled (JM) microparticles were determined via scanning electron microscopy, atomic force microscopy, dynamic light scattering particle size analysis, Karl Fischer titration, surface analysis, pycnometry, differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy. The in vitro aerosol dispersion performance and drug dissolution behavior were evaluated using an Anderson cascade impactor and a Franz diffusion cell, respectively. The JM microparticles exhibited an irregular corrugated surface and a crystalline solid state, while the SD microparticles were spherical with a smooth surface and an amorphous solid state. Thus, the in vitro aerosol dispersion performance and dissolution behavior as DPIs were considerably different due to the differences in the physicochemical properties of the SD and JM microparticles. In particular, the highest grinding pressures under jet milling exhibited excellent aerosol dispersion performance with statistically higher values of 56.8%±2.0% of respirable fraction and 33.8%±2.3% of fine particle fraction and lower mass median aerodynamic diameter of 5.0±0.3 μm than the others (P<0.05, analysis of variance/Tukey). The drug dissolution mechanism was also affected by the physicochemical properties that determine the dissolution kinetics of the SD and JM microparticles, which were well fitted into the Higuchi and zero-order models, respectively.

Authors+Show Affiliations

College of Pharmacy, Chungbuk National University.College of Pharmacy, Chungbuk National University.College of Pharmacy, Chungbuk National University.Department of Pharmaceutical Engineering, Cheongju University, Cheongju.College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju.College of Pharmacy, Woosuk University, Wanju-gun.School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea.College of Pharmacy, Chungbuk National University.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28008226

Citation

Lee, Hyo-Jung, et al. "Preparation and Physicochemical Characterization of Spray-dried and Jet-milled Microparticles Containing Bosentan Hydrate for Dry Powder Inhalation Aerosols." Drug Design, Development and Therapy, vol. 10, 2016, pp. 4017-4030.
Lee HJ, Kang JH, Lee HG, et al. Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols. Drug Des Devel Ther. 2016;10:4017-4030.
Lee, H. J., Kang, J. H., Lee, H. G., Kim, D. W., Rhee, Y. S., Kim, J. Y., Park, E. S., & Park, C. W. (2016). Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols. Drug Design, Development and Therapy, 10, 4017-4030. https://doi.org/10.2147/DDDT.S120356
Lee HJ, et al. Preparation and Physicochemical Characterization of Spray-dried and Jet-milled Microparticles Containing Bosentan Hydrate for Dry Powder Inhalation Aerosols. Drug Des Devel Ther. 2016;10:4017-4030. PubMed PMID: 28008226.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and physicochemical characterization of spray-dried and jet-milled microparticles containing bosentan hydrate for dry powder inhalation aerosols. AU - Lee,Hyo-Jung, AU - Kang,Ji-Hyun, AU - Lee,Hong-Goo, AU - Kim,Dong-Wook, AU - Rhee,Yun-Seok, AU - Kim,Ju-Young, AU - Park,Eun-Seok, AU - Park,Chun-Woong, Y1 - 2016/12/13/ PY - 2016/12/24/entrez PY - 2016/12/23/pubmed PY - 2017/5/10/medline KW - bosentan KW - dry powder inhalations KW - jet milling KW - pulmonary arterial hypertension KW - respiratory drug delivery KW - spray drying SP - 4017 EP - 4030 JF - Drug design, development and therapy JO - Drug Des Devel Ther VL - 10 N2 - The objectives of this study were to prepare bosentan hydrate (BST) microparticles as dry powder inhalations (DPIs) via spray drying and jet milling under various parameters, to comprehensively characterize the physicochemical properties of the BST hydrate microparticles, and to evaluate the aerosol dispersion performance and dissolution behavior as DPIs. The BST microparticles were successfully prepared for DPIs by spray drying from feeding solution concentrations of 1%, 3%, and 5% (w/v) and by jet milling at grinding pressures of 2, 3, and 4 MPa. The physicochemical properties of the spray-dried (SD) and jet-milled (JM) microparticles were determined via scanning electron microscopy, atomic force microscopy, dynamic light scattering particle size analysis, Karl Fischer titration, surface analysis, pycnometry, differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy. The in vitro aerosol dispersion performance and drug dissolution behavior were evaluated using an Anderson cascade impactor and a Franz diffusion cell, respectively. The JM microparticles exhibited an irregular corrugated surface and a crystalline solid state, while the SD microparticles were spherical with a smooth surface and an amorphous solid state. Thus, the in vitro aerosol dispersion performance and dissolution behavior as DPIs were considerably different due to the differences in the physicochemical properties of the SD and JM microparticles. In particular, the highest grinding pressures under jet milling exhibited excellent aerosol dispersion performance with statistically higher values of 56.8%±2.0% of respirable fraction and 33.8%±2.3% of fine particle fraction and lower mass median aerodynamic diameter of 5.0±0.3 μm than the others (P<0.05, analysis of variance/Tukey). The drug dissolution mechanism was also affected by the physicochemical properties that determine the dissolution kinetics of the SD and JM microparticles, which were well fitted into the Higuchi and zero-order models, respectively. SN - 1177-8881 UR - https://www.unboundmedicine.com/medline/citation/28008226/Preparation_and_physicochemical_characterization_of_spray_dried_and_jet_milled_microparticles_containing_bosentan_hydrate_for_dry_powder_inhalation_aerosols_ L2 - https://dx.doi.org/10.2147/DDDT.S120356 DB - PRIME DP - Unbound Medicine ER -