Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations

© 2017, Springer Science+Business Media, LLC, part of Springer Nature. Purpose: This study aims to investigate the influence of different storage humidity conditions on crystallization and aerosol performance of inhalable spray dried amorphous powder formulations (Ciprofloxacin hydrochloride as the...

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Main Authors: Shetty, N., Zeng, L., Mangal, S., Nie, H., Rowles, Matthew, Guo, R., Han, Y., Park, J., Zhou, Q.
Format: Journal Article
Published: AAPS 2018
Online Access:http://hdl.handle.net/20.500.11937/65842
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author Shetty, N.
Zeng, L.
Mangal, S.
Nie, H.
Rowles, Matthew
Guo, R.
Han, Y.
Park, J.
Zhou, Q.
author_facet Shetty, N.
Zeng, L.
Mangal, S.
Nie, H.
Rowles, Matthew
Guo, R.
Han, Y.
Park, J.
Zhou, Q.
author_sort Shetty, N.
building Curtin Institutional Repository
collection Online Access
description © 2017, Springer Science+Business Media, LLC, part of Springer Nature. Purpose: This study aims to investigate the influence of different storage humidity conditions on crystallization and aerosol performance of inhalable spray dried amorphous powder formulations (Ciprofloxacin hydrochloride as the model drug). Methods: The spray dried samples were stored at 20%, 55% and 75% relative humidity (RH). Crystallinity was monitored by Powder X-ray diffraction (PXRD), and particle morphology was measured by scanning electron microscopy (SEM) and atomic force microscopy (AFM). Aerosol performance was evaluated using a multi-stage liquid impinger (MSLI). Results: PXRD diffractograms showed the spray dried Ciprofloxacin stored at 20% RH for three weeks were amorphous; whereas those stored at 55% RH and 75% RH started crystallizing after one hour. Fine particle fraction (FPF) of the particles was improved from 28% to 42% after storage at 55% RH for three days. Such improvement was attributed to the crystallization of amorphous powders, which led to increased particle roughness and reduced particulate contact area, as visualized by SEM and quantified by AFM. A linear relationship was observed between degree of crystallinity/crystallite size and FPF (R 2 = 0.94 and R 2 = 0.96, respectively). However, deterioration in aerosol performance was observed after storage at 75% RH due to formation of inter-particulate liquid/solid bridges, as confirmed by SEM. Conclusions: This study provides a fundamental understanding in moisture-induced physical and aerosol instability of the spray dried powder formulations.
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spelling curtin-20.500.11937-658422019-07-08T06:31:32Z Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations Shetty, N. Zeng, L. Mangal, S. Nie, H. Rowles, Matthew Guo, R. Han, Y. Park, J. Zhou, Q. © 2017, Springer Science+Business Media, LLC, part of Springer Nature. Purpose: This study aims to investigate the influence of different storage humidity conditions on crystallization and aerosol performance of inhalable spray dried amorphous powder formulations (Ciprofloxacin hydrochloride as the model drug). Methods: The spray dried samples were stored at 20%, 55% and 75% relative humidity (RH). Crystallinity was monitored by Powder X-ray diffraction (PXRD), and particle morphology was measured by scanning electron microscopy (SEM) and atomic force microscopy (AFM). Aerosol performance was evaluated using a multi-stage liquid impinger (MSLI). Results: PXRD diffractograms showed the spray dried Ciprofloxacin stored at 20% RH for three weeks were amorphous; whereas those stored at 55% RH and 75% RH started crystallizing after one hour. Fine particle fraction (FPF) of the particles was improved from 28% to 42% after storage at 55% RH for three days. Such improvement was attributed to the crystallization of amorphous powders, which led to increased particle roughness and reduced particulate contact area, as visualized by SEM and quantified by AFM. A linear relationship was observed between degree of crystallinity/crystallite size and FPF (R 2 = 0.94 and R 2 = 0.96, respectively). However, deterioration in aerosol performance was observed after storage at 75% RH due to formation of inter-particulate liquid/solid bridges, as confirmed by SEM. Conclusions: This study provides a fundamental understanding in moisture-induced physical and aerosol instability of the spray dried powder formulations. 2018 Journal Article http://hdl.handle.net/20.500.11937/65842 10.1007/s11095-017-2281-5 AAPS restricted
spellingShingle Shetty, N.
Zeng, L.
Mangal, S.
Nie, H.
Rowles, Matthew
Guo, R.
Han, Y.
Park, J.
Zhou, Q.
Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title_full Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title_fullStr Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title_full_unstemmed Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title_short Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations
title_sort effects of moisture-induced crystallization on the aerosol performance of spray dried amorphous ciprofloxacin powder formulations
url http://hdl.handle.net/20.500.11937/65842