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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 study
ID
Mitrović, Jelena R.
(
Avtor
),
ID
Bjelošević Žiberna, Maja
(
Avtor
),
ID
Ahlin Grabnar, Pegi
(
Avtor
),
ID
Planinšek, Odon
(
Avtor
),
ID
Savić, Snežana D.
(
Avtor
), et al.
PDF - Predstavitvena datoteka,
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(4,20 MB)
MD5: 125EBEF51E34FB5A229A6AAE3E163FA8
URL - Izvorni URL, za dostop obiščite
https://www.sciencedirect.com/science/article/pii/S0928098723001872
Galerija slik
Izvleček
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.
Jezik:
Angleški jezik
Ključne besede:
pyrazoloquinolinone
,
nanocrystals
,
freeze-drying
,
sucrose
,
trehalose
,
mannitol
Vrsta gradiva:
Članek v reviji
Tipologija:
1.01 - Izvirni znanstveni članek
Organizacija:
FFA - Fakulteta za farmacijo
Status publikacije:
Objavljeno
Različica publikacije:
Objavljena publikacija
Leto izida:
2023
Št. strani:
12 str.
Številčenje:
Vol. 189, art. 106557
PID:
20.500.12556/RUL-148364
UDK:
66.017-022.513.2:620.3
ISSN pri članku:
0928-0987
DOI:
10.1016/j.ejps.2023.106557
COBISS.SI-ID:
161164291
Datum objave v RUL:
18.08.2023
Število ogledov:
1004
Število prenosov:
44
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Objavi na:
Gradivo je del revije
Naslov:
European Journal of Pharmaceutical Sciences
Skrajšan naslov:
Eur. j. pharm. sci.
Založnik:
Elsevier
ISSN:
0928-0987
COBISS.SI-ID:
17553413
Licence
Licenca:
CC BY-NC-ND 4.0, Creative Commons Priznanje avtorstva-Nekomercialno-Brez predelav 4.0 Mednarodna
Povezava:
http://creativecommons.org/licenses/by-nc-nd/4.0/deed.sl
Opis:
Najbolj omejujoča licenca Creative Commons. Uporabniki lahko prenesejo in delijo delo v nekomercialne namene in ga ne smejo uporabiti za nobene druge namene.
Sekundarni jezik
Jezik:
Slovenski jezik
Ključne besede:
pirazolokinolinon
,
nanokristali
,
liofilizacija
,
saharoza
,
trehaloza
,
manitol
,
farmacevtske oblike
,
nanomateriali
Projekti
Financer:
Drugi - Drug financer ali več financerjev
Program financ.:
Science Fund of the Republic of Serbia
Številka projekta:
7749108
Naslov:
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
Akronim:
NanoCellEmoCog
Financer:
NIH - National Institutes of Health
Številka projekta:
R01 NS076517
Financer:
NIH - National Institutes of Health
Številka projekta:
R01 MH096463
Financer:
NSF - National Science Foundation
Program financ.:
Division of Chemistry
Številka projekta:
CHE-1625735
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