Physicochemical Characterization and Water Vapor Sorption of Organic Solution Advanced Spray-Dried Inhalable Trehalose Microparticles and Nanoparticles for Targeted Dry Powder Pulmonary Inhalation Delivery |
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Authors: | Xiaojian Li Heidi M Mansour |
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Institution: | (1) Department of Pharmaceutical Sciences—Drug Development Division, University of Kentucky College of Pharmacy, 789 S. Limestone Street, Lexington, Kentucky 40536-0596, USA; |
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Abstract: | Novel advanced spray-dried inhalable trehalose microparticulate/nanoparticulate powders with low water content were successfully
produced by organic solution advanced spray drying from dilute solution under various spray-drying conditions. Laser diffraction
was used to determine the volumetric particle size and size distribution. Particle morphology and surface morphology was imaged
and examined by scanning electron microscopy. Hot-stage microscopy was used to visualize the presence/absence of birefringency
before and following particle engineering design pharmaceutical processing, as well as phase transition behavior upon heating.
Water content in the solid state was quantified by Karl Fisher (KF) coulometric titration. Solid-state phase transitions and
degree of molecular order were examined by differential scanning calorimetry (DSC) and powder X-ray diffraction, respectively.
Scanning electron microscopy showed a correlation between particle morphology, surface morphology, and spray drying pump rate.
All advanced spray-dried microparticulate/nanoparticulate trehalose powders were in the respirable size range and exhibited
a unimodal distribution. All spray-dried powders had very low water content, as quantified by KF. The absence of crystallinity
in spray-dried particles was reflected in the powder X-ray diffractograms and confirmed by thermal analysis. DSC thermal analysis
indicated that the novel advanced spray-dried inhalable trehalose microparticles and nanoparticles exhibited a clear glass
transition (T
g). This is consistent with the formation of the amorphous glassy state. Spray-dried amorphous glassy trehalose inhalable microparticles
and nanoparticles exhibited vapor-induced (lyotropic) phase transitions with varying levels of relative humidity as measured
by gravimetric vapor sorption at 25°C and 37°C. |
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Keywords: | |
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