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Particle Characterization Of Poorly Water-soluble Drugs Using A Spray Freeze Drying Technique.

M. Kondo, T. Niwa, H. Okamoto, K. Danjo
Published 2009 · Chemistry, Medicine

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A spray freeze drying (SFD) method was developed to prepare the composite particles of poorly water-soluble drug. The aqueous solution dissolved drug and the functional polymer was sprayed directly into liquid nitrogen. Then, the iced droplets were lyophilized with freeze-dryer to prepare solid particles. Tolbutamide (TBM) and hydroxypropylmethylcellulose (HPMC) were used as a model drug and water-soluble polymeric carrier in this study, respectively. The morphological observation of particles revealed that the spherical particles having porous structure could be obtained by optimizing the loading amount of drug and polymer in the spray solution. Especially, SFD method was characterized that the prepared particles had significantly larger specific surface area comparing with those prepared by the standard spray drying technique. The physicochemical properties of the resultant particles were found to be dependent on the concentration of spray solution. When the solution with high content of drug and polymer was used, the particle size of the resulting composite particles increased and they became spherical. The specific surface area of the particles also increased as a result of higher concentration of solution. The evaluation of spray solution indicated that these results were dependent on the viscosity of spray solution. In addition, when composite particles of TBM were prepared using the SFD method with HPMC as a carrier, the crystallinity of TBM decreased as the proportion of HPMC increased. When the TBM : HPMC ratio reached 1 : 5, the crystallinity of the particles completely disappeared. The dissolution tests showed that the release profiles of poorly water-soluble TBM from SFD composite particles were drastically improved compared to bulk TBM. The 70% release time T(70) of composite particles prepared by the SFD method in a solution of pH 1.2 was quite smaller than that of bulk TBM, while in a solution of pH 6.8, it was slightly lower. In addition, the release rates were faster than those of standard spray dried (SD) composite particles for solutions of pH 1.2 and 6.8, respectively. When composite particles were prepared from mixtures with various composition ratios, T(70) was found to decrease as the proportion of HPMC increased; the release rate was faster than that of bulk TBM in a solution of pH 6.8, as well as solution of pH 1.2.
This paper references
10.1016/S0378-5173(97)00101-4
Investigation of the triamterene-β-cyclodextrin system prepared by co-grinding
M. Arias (1997)
10.1016/0378-5173(92)90100-G
Mucoadhesion of both film-forming and non-film-forming polymeric materials as evaluated with the Wilhelmy plate method
A. P. Sam (1992)
10.1016/S0378-5173(00)00423-3
Lyophilization and development of solid protein pharmaceuticals.
W. Wang (2000)
10.1023/A:1022628826404
Enhanced Aqueous Dissolution of a Poorly Water Soluble Drug by Novel Particle Engineering Technology: Spray-Freezing into Liquid with Atmospheric Freeze-Drying
T. L. Rogers (2004)
10.1016/S0928-0987(03)00203-3
Spray freezing into liquid (SFL) particle engineering technology to enhance dissolution of poorly water soluble drugs: organic solvent versus organic/aqueous co-solvent systems.
Jiahui Hu (2003)
10.1248/CPB.52.1066
Improved dissolution of an insoluble drug using a 4-fluid nozzle spray-drying technique.
R. Chen (2004)
10.1002/JPS.2600830425
Improved oral absorption of enteric coprecipitates of a poorly soluble drug.
N. Kondo (1994)
10.1016/J.IJPHARM.2005.06.027
Stabilizer choice for rapid dissolving high potency itraconazole particles formed by evaporative precipitation into aqueous solution.
Prapasri Sinswat (2005)
10.1021/JS980376Z
Characterization of tolbutamide polymorphs (Burger's forms II and IV) and polymorphic transition behavior.
K. Kimura (1999)
10.1016/S0939-6411(02)00063-2
A novel particle engineering technology to enhance dissolution of poorly water soluble drugs: spray-freezing into liquid.
T. L. Rogers (2002)
10.1016/S0939-6411(02)00050-4
Preparation and characterization of microparticles containing peptide produced by a novel process: spray freezing into liquid.
Zhongshui Yu (2002)
10.1248/CPB.45.1840
Preparation and Dissolution Behavior of Ethenzamide Solid Dispersions Using Various Sugars as Dispersion Carriers
K. Danjo (1997)
10.1016/S0378-5173(02)00154-0
A novel particle engineering technology: spray-freezing into liquid.
T. L. Rogers (2002)
10.1023/A:1020390422785
Improvement of Dissolution Rates of Poorly Water Soluble APIs Using Novel Spray Freezing into Liquid Technology
Jiahui Hu (2004)
Release Profiles of Samples (a) pH
K. Kimura (1999)



This paper is referenced by
10.1016/j.ijpharm.2011.09.003
Process optimization of a novel production method for nanosuspensions using design of experiments (DoE).
J. Salazar (2011)
10.1016/j.ejpb.2011.12.015
Nanocrystals: comparison of the size reduction effectiveness of a novel combinative method with conventional top-down approaches.
J. Salazar (2012)
10.1016/J.JDDST.2015.07.021
Fabrication of aceclofenac nanocrystals for improved dissolution: Process optimization and physicochemical characterization
Satyanarayan Pattnaik (2015)
10.1016/J.POWTEC.2014.03.043
Inhalable budesonide porous microparticles tailored by spray freeze drying technique
A. Parsian (2014)
10.1016/j.heliyon.2020.e04589
Formulation of PPAR-gamma agonist as surface modified PLGA nanoparticles for non-invasive treatment of diabetic retinopathy: in vitro and in vivo evidences
Umesh D. Laddha (2020)
10.1002/btpr.618
Polymer‐based microparticles in tissue engineering and regenerative medicine
M. Oliveira (2011)
10.3390/pr8060709
Spray freeze-drying as a solution to continuous manufacturing of pharmaceutical products in bulk
M. B. Adalı (2020)
10.1517/17425247.2012.652614
Production methodologies of polymeric and hydrogel particles for drug delivery applications
A. C. Lima (2012)
10.1016/j.ijpharm.2010.06.016
Enhanced dissolution of megestrol acetate microcrystals prepared by antisolvent precipitation process using hydrophilic additives.
Eunbi Cho (2010)
10.1016/j.jconrel.2011.01.010
Development and characterization of Cyclosporine A loaded nanoparticles for ocular drug delivery: Cellular toxicity, uptake, and kinetic studies.
P. Aksungur (2011)
10.1016/j.ejps.2010.05.019
One-step preparation of pharmaceutical nanocrystals using ultra cryo-milling technique in liquid nitrogen.
T. Niwa (2010)
10.3109/02652048.2011.599442
Lipid–polymer composite microspheres for colon-specific drug delivery prepared using an ultrasonic spray freeze-drying technique
Yiping Gao (2011)
10.1016/j.ejps.2017.05.007
Large porous particles for respiratory drug delivery. Glycine‐based formulations
A. G. Ogienko (2017)
10.11606/T.60.2015.tde-12052015-114418
Sistemas microestruturados contendo extratos de Chamomilla recutita L. para aplicações dermocosméticas
Simone Vieira Pereira (2015)
10.1517/17425247.2011.598147
Improved dissolution behavior of lipophilic drugs by solid dispersions: the production process as starting point for formulation considerations
P. Srinarong (2011)
10.1002/jbm.b.33266
Fabrication of biodegradable polyurethane microspheres by a facile and green process.
Cheng-Yen Lin (2015)
10.1016/j.carbpol.2013.12.026
Agarose drug delivery systems upgraded by surfactants inclusion: critical role of the pore architecture.
T. Marras-Marquez (2014)
10.1517/17425247.2011.618181
Solid dispersions, Part I: recent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs
D. Bikiaris (2011)
10.1248/CPB.58.195
Novel spray freeze-drying technique using four-fluid nozzle-development of organic solvent system to expand its application to poorly water soluble drugs.
T. Niwa (2010)
10.1016/j.jconrel.2019.02.044
Spray freeze drying: Emerging applications in drug delivery.
D. Vishali (2019)
10.1016/j.ejps.2013.07.011
Design of self-dispersible dry nanosuspension through wet milling and spray freeze-drying for poorly water-soluble drugs.
T. Niwa (2013)
10.1016/j.ijpharm.2010.11.043
Solution interactions of diclofenac sodium and meclofenamic acid sodium with hydroxypropyl methylcellulose (HPMC).
S. Pygall (2011)
10.1248/YAKUSHI.131.711
[Dissolution characteristics of composite particles using a spray freeze drying].
M. Kondo (2011)
10.1016/j.ijpharm.2010.09.039
Inorganic-polymer nanohybrid carrier for delivery of a poorly-soluble drug, ursodeoxycholic acid.
G. Choi (2010)
10.1016/j.ijpharm.2015.04.053
Pharmaceutical spray freeze drying.
S. Wanning (2015)
10.11203/JAR.25.155
Preparations of Dry-Powder Therapeutic Nanoparticle Aerosols for Inhaled Drug Delivery
Wean Sin Cheow (2010)
Effect of whey protein isolate and b-cyclodextrin wall systems on stability of microencapsulated vanillin by spray–freeze drying method
Swetank Y. Hundre (2014)
10.22037/IJPR.2014.1530
Clarithromycin Dissolution Enhancement by Preparation of Aqueous Nanosuspensions Using Sonoprecipitation Technique
Es ׳hagh Esfandi (2014)
10.1155/2014/683153
Cyclosporine A Loaded PLGA Nanoparticles for Dry Eye Disease: In Vitro Characterization Studies
Vijay D. Wagh (2014)
10.1002/PPSC.201300298
A Simple, Scalable Process for the Production of Porous Polymer Microspheres by Ink‐Jetting Combined with Thermally Induced Phase Separation
Dewi P. Go (2014)
10.2165/11539070-000000000-00000
Systemic and Mucosal Delivery of Drugs within Polymeric Microparticles Produced by Spray Drying
K. Bowey (2012)
10.1016/j.foodchem.2014.11.016
Effect of whey protein isolate and β-cyclodextrin wall systems on stability of microencapsulated vanillin by spray-freeze drying method.
Swetank Y. Hundre (2015)
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