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Ibuprofen nanocrystals developed by 2(2) factorial design experiment: A new approach for poorly water-soluble drugs

Title
Ibuprofen nanocrystals developed by 2(2) factorial design experiment: A new approach for poorly water-soluble drugs
Type
Article in International Scientific Journal
Year
2017
Authors
Fernandes, AR
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Ferreira, NR
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Fangueiro, JF
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Santos, AC
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Veiga, FJ
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Cabral, C
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Silva, AM
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Souto, EB
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Journal
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Vol. 25
Pages: 1117-1124
ISSN: 1319-0164
Other information
Authenticus ID: P-00N-NTZ
Abstract (EN): The reduction of the particle size of drugs of pharmaceutical interest down to the nano-sized range has dramatically changed their physicochemical properties. The greatest disadvantage of nanocrystals is their inherent instability, due to the risk of crystal growth. Thus, the selection of an appropriate stabilizer is crucial to obtain long-term physicochemically stable nanocrystals. High pressure homogenization has enormous advantages, including the possibility of scaling up, lack of organic solvents and the production of small particles diameter with low polydispersity index. The sequential use of high shear homogenization followed by high pressure homogenization, can modulate nanoparticles' size for different administration routes. The present study focuses on the optimization of the production process of two formulations composed of different surfactants produced by High Shear Homogenization followed by hot High Pressure Homogenization. To build up the surface response charts, a 2(2) full factorial design experiment, based on 2 independent variables, was used to develop optimized formulations. The effects of the production process on the mean particle size and polydispersity index were evaluated. The best ibuprofen nanocrystal formulations were obtained using 0.20% Tween 80 and 1.20% PVP K30 (F1) and 0.20% Tween 80 and 1.20% Span 80 (F2). The estimation of the long-term stability of the aqueous suspensions of ibuprofen nanocrystals was studied using the LUMISizer. The calculated instability index suggests that F1 was more stable when stored at 4 degrees C and 22 degrees C, whereas F2 was shown to be more stable when freshly prepared. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 8
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