Nanocrystal dispersion of DK-I-56–1, a poorly soluble pyrazoloquinolinone positive modulator of α6 GABAA receptors: Formulation approach toward improved in vivo performance
| Autor: | Snežana Savić, Miroslav M. Savić, James M. Cook, Predrag Vulić, Vladimir Dobričić, Branka Divović, Jelena Đoković, Daniel E. Knutson, Jelena R Mitrović, Danijela Randjelovic, Bojan Čalija |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Biodistribution
Dispersity Pharmaceutical Science 02 engineering and technology Polyethylene glycol Quinolones 030226 pharmacology & pharmacy Pyrazoloquinolinones Article 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine Suspensions Wet ball milling In vivo Animals Tissue Distribution Pharmacokinetics Particle Size Poloxamer 021001 nanoscience & nanotechnology Receptors GABA-A Combinatorial chemistry 3. Good health Bioavailability chemistry Nanocrystal Solubility Pharmacodynamics Nanosuspension Nanoparticles Pyrazoles Particle size 0210 nano-technology |
| Zdroj: | European Journal of Pharmaceutical Science Eur J Pharm Sci European Journal of Pharmaceutical Sciences |
| Popis: | DK-I-56–1 (7‑methoxy‑2-(4‑methoxy‑d3-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one), a recently developed deuterated pyrazoloquinolinone, has been recognized as a lead candidate for treatment of various neuropsychiatric disorders. During preclinical investigation of poorly water-soluble compounds such as DK-I-56–1, the application of nanotechnology could be advantageous due to improved safety and possibly increased bioavailability of nanosized formulation. DK-I-56–1 nanosuspensions stabilized by polysorbate 80, alone or in combination with poloxamers 188 i.e. 407 or D-α-tocopheryl polyethylene glycol 1000 succinate, were prepared using a small-scale media milling device. With particle size 208.7–250.6 nm and polydispersity index |
| Databáze: | OpenAIRE |
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