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Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study
Despite of good pharmacodynamics of DK-I-56-1, novel deuterated pyrazoloquinolinones ligand, low solubility limits its administration. Nanosuspensions can help to overcome this problem, but its small particle size usually leads to particle agglomeration in short period of time. This phenomenon can be prevented by performing lyophilization. In this study cryoprotectants selection as well as characterization (particle size measurements after redispersion, scanning electron microscopy, differential scanning calorimetry and thermogravimetric measurements) of obtained freeze dried preparations was carried out. It was observed that sucrose/mannitol ratio 1:1 and 3:2 in total concentration of 10% can preserve particle size during lyophilization. However, after stability study conducted during one month storage at 25 °C and 40 °C, particle size remained in submicron range only in one sample. Changes in particle size were also followed by changes in polymorphic form of mannitol. It can be concl...uded that changes of crystal forms in freeze dried preparations during storage could jeopardize their stability, and therefore should be carefully examined.
CEEPUS project CIII-RS-1113-02-1819-M-118533 - Central European Knowledge Alliance for Teaching, Learning & Research in Pharmaceutical Technology (CEKA PharmTech).
TY - CONF
AU - Mitrović, Jelena
AU - Bjelošević, Maja
AU - Đoković, Jelena
AU - Ahlin Grabnar, Pegi
AU - Planinšek, Odon
AU - Knutson, Daniel
AU - Cook, James
AU - Savić, Miroslav
AU - Savić, Snežana
PY - 2020
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3744
AB - Despite of good pharmacodynamics of DK-I-56-1, novel deuterated pyrazoloquinolinones ligand, low solubility limits its administration. Nanosuspensions can help to overcome this problem, but its small particle size usually leads to particle agglomeration in short period of time. This phenomenon can be prevented by performing lyophilization. In this study cryoprotectants selection as well as characterization (particle size measurements after redispersion, scanning electron microscopy, differential scanning calorimetry and thermogravimetric measurements) of obtained freeze dried preparations was carried out. It was observed that sucrose/mannitol ratio 1:1 and 3:2 in total concentration of 10% can preserve particle size during lyophilization. However, after stability study conducted during one month storage at 25 °C and 40 °C, particle size remained in submicron range only in one sample. Changes in particle size were also followed by changes in polymorphic form of mannitol. It can be concluded that changes of crystal forms in freeze dried preparations during storage could jeopardize their stability, and therefore should be carefully examined.
T1 - Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study
ER -
@conference{
author = "Mitrović, Jelena and Bjelošević, Maja and Đoković, Jelena and Ahlin Grabnar, Pegi and Planinšek, Odon and Knutson, Daniel and Cook, James and Savić, Miroslav and Savić, Snežana",
year = "2020",
url = "https://farfar.pharmacy.bg.ac.rs/handle/123456789/3744",
abstract = "Despite of good pharmacodynamics of DK-I-56-1, novel deuterated pyrazoloquinolinones ligand, low solubility limits its administration. Nanosuspensions can help to overcome this problem, but its small particle size usually leads to particle agglomeration in short period of time. This phenomenon can be prevented by performing lyophilization. In this study cryoprotectants selection as well as characterization (particle size measurements after redispersion, scanning electron microscopy, differential scanning calorimetry and thermogravimetric measurements) of obtained freeze dried preparations was carried out. It was observed that sucrose/mannitol ratio 1:1 and 3:2 in total concentration of 10% can preserve particle size during lyophilization. However, after stability study conducted during one month storage at 25 °C and 40 °C, particle size remained in submicron range only in one sample. Changes in particle size were also followed by changes in polymorphic form of mannitol. It can be concluded that changes of crystal forms in freeze dried preparations during storage could jeopardize their stability, and therefore should be carefully examined.",
title = "Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study"
}
Mitrović J, Bjelošević M, Đoković J, Ahlin Grabnar P, Planinšek O, Knutson D, Cook J, Savić M, Savić S. Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study. 2020;
Mitrović, J., Bjelošević, M., Đoković, J., Ahlin Grabnar, P., Planinšek, O., Knutson, D., Cook, J., Savić, M.,& Savić, S. (2020). Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study.
.
Mitrović Jelena, Bjelošević Maja, Đoković Jelena, Ahlin Grabnar Pegi, Planinšek Odon, Knutson Daniel, Cook James, Savić Miroslav, Savić Snežana, "Nanosuspensions of novel deuterated pyrazoloquinolinones ligand (DK-I-56-1): lyophilization procedure development through cryoprotectant selection and stability study" (2020)
