| People | Locations | Statistics |
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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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Müllertz, Anette
University of Copenhagen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (18/18 displayed)
- 2024Influence of preparation method and choice of phospholipid on co-amorphization, physical stability, and dissolution behavior of equimolar indomethacin-phospholipid systemscitations
- 2024Drug–Phospholipid Co-Amorphous Formulations: The Role of Preparation Methods and Phospholipid Selection
- 2023Amphotericin B and monoacyl-phosphatidylcholine form a stable amorphous complexcitations
- 2023Stability and intrinsic dissolution of vacuum compression molded amorphous solid dispersions of efavirenzcitations
- 2023Coating of Primary Powder Particles Improves the Quality of Binder Jetting 3D Printed Oral Solid Productscitations
- 2022Structured approach for designing drug-loaded solid products by binder jetting 3D printingcitations
- 2021Hot punching for loading of biodegradable microcontainers with budesonide-Soluplus filmcitations
- 2018The Influence of Polymers on the Supersaturation Potential of Poor and Good Glass Formerscitations
- 2016In Vivo Precipitation of Poorly Soluble Drugs from Lipid-Based Drug Delivery Systemscitations
- 2016Supersaturation of zafirlukast in fasted and fed state intestinal media with and without precipitation inhibitorscitations
- 2015Stabilisation of amorphous furosemide increases the oral drug bioavailability in ratscitations
- 2014Physical characterization of photocrosslinked poly(vinyl pyrrolidone) (PVP) hydrogels for drug delivery
- 2014Property profiling of biosimilar mucus in a novel mucus-containing in vitro model for assessment of intestinal drug absorptioncitations
- 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.
- 2010Precipitation of a poorly soluble model drug during in vitro lilpolysiscitations
- 2008Characterization and physical stability of spray dried solid dispersions of probucol and PVP-K30citations
Places of action
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article
Amphotericin B and monoacyl-phosphatidylcholine form a stable amorphous complex
Abstract
<p>Amphotericin B (AmB) is a “life-saving” medicine for the treatment of invasive fungal infections and visceral leishmaniasis. To date, all marketed AmB formulations require parenteral administration, which causes high rates of acute infusion-related side effects and dose-dependent nephrotoxicity. The development of an oral AmB formulation will entail numerous advantages including increased patient compliance, eliminated infusion-related toxicities and reduced nephrotoxicity. Unfortunately, the gastrointestinal absorption of AmB is negligible due to its extremely low solubility in both aqueous and lipid solvents, and its poor gastrointestinal permeability. Drug-phospholipid complexation is an emerging strategy for oral delivery of poorly soluble drugs. In this study, monoacyl-phosphatidylcholine (MAPC) was complexed with AmB forming an AmB-MAPC complex (APC), to enhance the dissolution rate and aqueous solubility of AmB, in order to enable oral delivery of AmB. X-ray powder diffraction demonstrated that AmB was transformed to its amorphous form following complexation with MAPC, i.e. in the APC. Fourier-transform infrared spectroscopy suggested molecular interactions between AmB and MAPC. Dynamic light scattering indicated formation of colloidal structures after aqueous dispersion of APC; Cryogenic transmission electron microscopy showed that APC formed small round, “rod-like” and “worm-like” micellar structures and Small-angle neutron scattering provided three-dimensional micellar structures formed by APC upon aqueous dispersion, which indicated that AmB was inserted into the micellar mono-layer membrane formed by MAPC. Additionally, APC showed an increased dissolution rate and a higher amount of AmB solubilized in fasted state simulated intestinal fluid, compared to AmB/MAPC physical mixtures and crystalline AmB. In conclusion, an APC exhibiting amorphous properties was developed, the APC showed improved dissolution rate and increased apparent aqueous solubility compared to AmB, indicating that the application of APC could be a promising strategy to enable the oral delivery of AmB.</p>