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Naji, M. |
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Motta, Antonella |
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Aletan, Dirar |
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Mohamed, Tarek |
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Ertürk, Emre |
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Taccardi, Nicola |
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Kononenko, Denys |
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Petrov, R. H. | Madrid |
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Alshaaer, Mazen | Brussels |
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Bih, L. |
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Casati, R. |
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Muller, Hermance |
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Kočí, Jan | Prague |
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Šuljagić, Marija |
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Kalteremidou, Kalliopi-Artemi | Brussels |
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Azam, Siraj |
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Ospanova, Alyiya |
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Blanpain, Bart |
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Ali, M. A. |
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Popa, V. |
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Rančić, M. |
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Ollier, Nadège |
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Azevedo, Nuno Monteiro |
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Landes, Michael |
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Rignanese, Gian-Marco |
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Nielsen, Line Hagner
Technical University of Denmark
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (12/12 displayed)
- 20233D-printed Radiopaque Microdevices with Enhanced Mucoadhesive Geometry for Oral Drug Deliverycitations
- 2019Artificial gut-on-a-disc platform to evaluate ph sensitive coatings of oral drug delivery devices
- 2019Where Is the Drug? Quantitative 3D Distribution Analyses of Confined Drug-Loaded Polymer Matricescitations
- 2019Evaluation of the solid state form of tadalafil in sub-micron thin films using nanomechanical infrared spectroscopycitations
- 2018Evaluation of the effects of spray drying parameters for producing cubosome powder precursorscitations
- 2018Evaluation of the effects of spray drying parameters for producing cubosome powder precursorscitations
- 2017Microcontainers as an oral delivery system for spray dried cubosomes containing ovalbumincitations
- 2016Triple co-culture cell model as an in vitro model for oral particulate vaccine systems
- 2015Stabilisation of amorphous furosemide increases the oral drug bioavailability in ratscitations
- 2013Spray coating of microcontainers with eudragit using ferromagnetic shadow masks for controlled oral release of poorly water soluble drugs.
- 2013Preparation of an amorphous sodium furosemide salt improves solubility and dissolution rate and leads to a faster Tmax after oral dosing to ratscitations
- 2013Biodegradable microcontainers as an oral drug delivery system for poorly soluble drugs.
Places of action
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article
Where Is the Drug? Quantitative 3D Distribution Analyses of Confined Drug-Loaded Polymer Matrices
Abstract
To enhance oral bioavailability of poorly soluble drugs, microfabricated devices can be utilized. One example of such devices is microcontainers. These are cylindrical in shape with an inner cavity for drug loading and with only the top side open for release. Supercritical CO<sub>2</sub> (scCO<sub>2</sub>) impregnation is an interesting technique for loading drugs into polymeric matrices in, for example, microcontainers since it avoids the use of organic solvents and is cheap. One of the main drawbacks of this technique is the unknown three-dimensional drug distribution in the polymer matrix. The aim of this study was to investigate the loading of two poorly soluble drugs, naproxen and ketoprofen, by scCO<sub>2</sub> impregnation into confined polymermatrices of different sizes. Three different sizes of microcontainers (small, medium, and large) and, thereby, different surface areas accessible for impregnation were compared. From in vitro studies, the amount of naproxen and ketoprofen loaded into the different microcontainers and their corresponding release profiles were seen to be similar. A custom-made Raman microscope facilitated volumetric Raman maps of an entire microcontainer filled with polyvinylpyrrolidone (PVP) and scCO<sub>2</sub> impregnated with either naproxen or ketoprofen. In all microcontainer sizes, the drugs were only detected in the top layer of the polymer matrix, explaining the observed similar release profiles. Using X-ray powder diffraction and Raman spectroscopy, the solid state form of the drugs was evaluated, showing that ketoprofen was amorphous in all microcontainer sizes. Naproxen was found not to be crystalline nor amorphous but in a less ordered configuration than the crystalline state. In conclusion, volumetric Raman mapping is a powerful technology for imaging drug distribution and drug crystallinity in polymers and allowed us to conclude that (i) scCO<sub>2</sub> impregnation depth does not depend on surface area and (ii) impregnated drugs are noncrystalline.