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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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Liu, M.
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (12/12 displayed)
- 2025Surface Modified CsPbBr3 Nanocrystals Enable Free Radical Thermal Polymerization of Efficient Ultrafast Polystirenic Nanocomposite Scintillatorscitations
- 2024Halide Engineering in Mixed Halide Perovskite-Inspired Cu2AgBiI6 for Solar Cells with Enhanced Performancecitations
- 2023Corrosion and passive film characteristics of 3D-printed NiTi shape memory alloys in artificial salivacitations
- 2023Passive film formation and corrosion resistance of laser-powder bed fusion fabricated NiTi shape memory alloyscitations
- 2021Positron annihilation investigation of thermal cycling induced martensitic transformation in NiTi shape memory alloycitations
- 2021The influence of zinc electrode substrate, electrolyte flow rate and current density on zinc-nickel flow cell performancecitations
- 2020Improving solubility and oral bioavailability of a novel antimalarial prodrug: comparing spray-dried dispersions with self-emulsifying drug delivery systems.citations
- 2019Fluoride-Salt-Cooled High-Temperature Reactor (FHR) Using British Advanced Gas-Cooled Reactor (AGR) Refueling Technology and Decay Heat Removal Systems That Prevent Salt Freezing
- 2019Characterization of native oxide and passive film on austenite/ferrite phases of duplex stainless steel using synchrotron haxpeemcitations
- 2016Efficient planar heterojunction perovskite solar cells by vapour deposition.citations
- 2016Efficient planar heterojunction perovskite solar cells by vapour depositioncitations
- 2015Charge selective contacts, mobile ions and anomalous hysteresis in organic-inorganic perovskite solar cellscitations
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article
Improving solubility and oral bioavailability of a novel antimalarial prodrug: comparing spray-dried dispersions with self-emulsifying drug delivery systems.
Abstract
To improve the solubility and oral bioavailability of a novel antimalarial agent ELQ-331(a prodrug of ELQ-300), spray-dried dispersions (SDD) and a self-emulsifying drug delivery system (SEDDS) were developed. SDD were prepared with polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus<sup>®</sup>) polymer carrier and Aeroperl<sup>®</sup> 300 Pharma and characterized by differential scanning calorimetry, powder X-ray diffraction. For SEDDS, solubility in oils, surfactants, and co-surfactants was determined and ternary phase diagram was constructed to show self-emulsifying area. SEDDS were characterized for spontaneous emulsification and droplet size distribution. The amorphous ELQ-331 SDD improved the solubility to 10× in fast-state simulated intestinal fluid and addition of sodium lauryl sulphate externally to SDDs further improved the solubility to ∼28.5× versus non-formulated drug. SEDDS had good self-emulsifying characteristics with small emulsion droplet sizes and narrow particle distribution. Oral pharmacokinetic studies for SDD and SEDDS formulations were performed in rats. The ELQ-331 rapidly converted to ELQ-300 soon after oral administration in rats. Exposure levels of ELQ-300 were about 1.4-fold higher (based on AUC) in SEDDS than SDD formulations. Poorly soluble drugs like ELQ-331 can be formulated using SDD or SEDDS to improve solubility and oral bioavailability.