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Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations.
Pharm Res. 2018 01 02; 35(1):7.PR

Abstract

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 (R2 = 0.94 and R2 = 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.

Links

Authors+Show Affiliations

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Teva Pharmaceuticals, 145 Brandywine Pkwy, West Chester, Pennsylvania, 19380, USA.

Department of Physics and Astronomy, Curtin University, Bentley, WA, 6102, Australia.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA.

Birck Nanotechnology Center, Purdue University, 1205 West State Street, West Lafayette, Indiana, 47907, USA.

Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana, 47907, USA. tonyzhou@purdue.edu.

MeSH

Administration, InhalationAerosolsCalorimetry, Differential ScanningChromatography, High Pressure LiquidCiprofloxacinCrystallizationDrug CompoundingHumansHumidityKineticsMicroscopy, Atomic ForceMicroscopy, Electron, ScanningParticle SizePowdersSteamSurface PropertiesX-Ray Diffraction

Pub Type(s)

Journal Article

Research Support, N.I.H., Extramural

Language

eng

PubMed ID

29294198

Citation

Shetty, Nivedita, et al. "Effects of Moisture-Induced Crystallization On the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations." Pharmaceutical Research, vol. 35, no. 1, 2018, p. 7.

Shetty N, Zeng L, Mangal S, et al. Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations. Pharm Res. 2018;35(1):7.

Shetty, N., Zeng, L., Mangal, S., Nie, H., Rowles, M. R., Guo, R., Han, Y., Park, J. H., & Zhou, Q. T. (2018). Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations. Pharmaceutical Research, 35(1), 7. https://doi.org/10.1007/s11095-017-2281-5

Shetty N, et al. Effects of Moisture-Induced Crystallization On the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations. Pharm Res. 2018 01 2;35(1):7. PubMed PMID: 29294198.

* Article titles in AMA citation format should be in sentence-case

TY - JOUR T1 - Effects of Moisture-Induced Crystallization on the Aerosol Performance of Spray Dried Amorphous Ciprofloxacin Powder Formulations. AU - Shetty,Nivedita, AU - Zeng,Lingfei, AU - Mangal,Sharad, AU - Nie,Haichen, AU - Rowles,Matthew R, AU - Guo,Rui, AU - Han,Youngwoo, AU - Park,Joon Hyeong, AU - Zhou,Qi Tony, Y1 - 2018/01/02/ PY - 2017/09/01/received PY - 2017/10/13/accepted PY - 2018/1/3/entrez PY - 2018/1/3/pubmed PY - 2018/11/13/medline KW - aerosol performance KW - amorphous powder KW - crystallization KW - dry powder inhaler KW - particle surface roughness KW - spray drying KW - storage humidity SP - 7 EP - 7 JF - Pharmaceutical research JO - Pharm Res VL - 35 IS - 1 N2 - 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 (R2 = 0.94 and R2 = 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. SN - 1573-904X UR - https://www.unboundmedicine.com/medline/citation/29294198/Effects_of_Moisture_Induced_Crystallization_on_the_Aerosol_Performance_of_Spray_Dried_Amorphous_Ciprofloxacin_Powder_Formulations_ DB - PRIME DP - Unbound Medicine ER -