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Freeze-dried nanocrystal dispersion of novel deuterated pyrazoloquinolinone ligand (DK-I-56-1) : process parameters and lyoprotectant selection through the stability studyMitrović, Jelena ...Recently, nanocrystal dispersions have been considered as a promising formulation strategy to improve the bioavailability of the deuterated pyrazoloquinolinone ligand DK-I-56-1 ... (7-methoxy-2-(4-methoxy-d3-phenyl)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one). In the current study, the freeze-drying process (formulation and process parameters) was investigated to improve the storage stability of the previously developed formulation. Different combinations of lyoprotectant (sucrose or trehalose) and bulking agent (mannitol) were varied while formulations were freeze-dried under two conditions (primary drying at -10°C or -45°C). The obtained lyophilizates were characterized in terms of particle size, solid state properties and morphology, while the interactions within the samples were analyzed by Fourier transform infrared spectroscopy. In the preliminary study, three formulations were selected based on the high redispersibility index values (around 95%). The temperature of primary drying had no significant effect on particle size, but stability during storage was impaired for samples dried at -10°C. Samples dried at lower temperature were more homogeneous and remained stable for three months. It was found that the optimal ratio of sucrose or trehalose to mannitol was 3:2 at a total concentration of 10% to achieve the best stability (particle size <1.0 μm, polydispersity index <0.250). The amorphous state of lyoprotectants probably provided a high degree of interaction with nanocrystals, while the crystalline mannitol provided an elegant cake structure. Sucrose was superior to trehalose in maintaining particle size during freeze-drying, while trehalose was more effective in keeping particle size within limits during storage. In conclusion, results demonstrated that the appropriate combination of sucrose/trehalose and mannitol together with the appropriate selection of lyophilization process parameters could yield nanocrystals with satisfactory stability.Vir: European Journal of Pharmaceutical Sciences. - ISSN 0928-0987 (Vol. 189, 2023, 12 str.)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2023Jezik - angleškiCOBISS.SI-ID - 161164291
Avtor
Mitrović, Jelena |
Bjelošević Žiberna, Maja |
Vukadinović, Aleksandar, farmacevt |
Knutson, Daniel E. |
Sharmin, Dishary |
Kremenović, Aleksandar |
Ahlin Grabnar, Pegi |
Planinšek, Odon |
Lunter, Dominique |
Savić, Snežana D.
Teme
Farmacevtske oblike |
Nanomateriali |
pyrazoloquinolinone |
nanocrystals |
freeze-drying |
sucrose |
trehalose |
mannitol |
pirazolokinolinon |
nanokristali |
liofilizacija |
saharoza |
trehaloza |
manitol
Avtor | Mitrović, Jelena ... |
Naslov | Freeze-dried nanocrystal dispersion of novel deuterated pyrazoloquinolinone ligand (DK-I-56-1) : process parameters and lyoprotectant selection through the stability study |
Datum objave | |
COBISS.SI-ID | 161164291 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
Neuroimmune aspects of mood, anxiety and cognitive effects of leads/drug candidates acting at GABAA and/or sigma-2 receptors: In vitro/in vivo delineation by nano- and hiPSC-based platforms-NanoCellEmoCog | 7749108 | ||
National Institutes of Health, USA | R01 NS076517 |
National Institutes of Health |
|
National Institutes of Health, USA | R01 MH096463 |
National Institutes of Health |
|
National Science Foundation, Division of Chemistry | CHE- 1625735 |
Datoteke, ki spadajo k objavi
Povezava |
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https://www.sciencedirect.com/science/article/pii/S0928098723001872 |
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=148364 |
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Mitrović, Jelena | |
Bjelošević Žiberna, Maja | 38497 |
Vukadinović, Aleksandar, farmacevt | |
Knutson, Daniel E. | |
Sharmin, Dishary | |
Kremenović, Aleksandar | |
Ahlin Grabnar, Pegi | 15490 |
Planinšek, Odon | 14935 |
Lunter, Dominique | |
Savić, Snežana D. |
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