Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocaine
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Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocaine. / Xu, Xiaoyue; Rades, Thomas; Grohganz, Holger.
In: International Journal of Pharmaceutics, Vol. 651, 123807, 2024.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocaine
AU - Xu, Xiaoyue
AU - Rades, Thomas
AU - Grohganz, Holger
N1 - Publisher Copyright: © 2024 The Author(s)
PY - 2024
Y1 - 2024
N2 - It is generally accepted that water as a plasticizer can decrease the glass transition temperatures (Tgs) of amorphous drugs and drug excipient systems. However, previous studies suggest that water, as an anti-plasticizer, can increase the Tgs of co-amorphous systems of prilocaine (PRL) and lidocaine (LID). In order to investigate the intermolecular interactions between water and co-amorphous PRL-LID systems, Fourier transform infrared spectroscopy (FTIR) and principal component analysis (PCA) were conducted. Water was found to bind with the carbonyl groups of PRL and LID molecularly evenly in the hydrated co-amorphous PRL-LID systems. Quantum chemical simulations visually confirmed the interactions between water and co-amorphous PRL-LID systems. Furthermore, the physical stability of hydrated co-amorphous PRL-LID systems was improved due to the anti-plasticizing effect of water, compared with the anhydrous samples. The preference of water to interact with the carbonyl groups of PRL and LID as binding sites could be associated with the anti-plasticizing effect of water on the co-amorphous PRL-LID systems.
AB - It is generally accepted that water as a plasticizer can decrease the glass transition temperatures (Tgs) of amorphous drugs and drug excipient systems. However, previous studies suggest that water, as an anti-plasticizer, can increase the Tgs of co-amorphous systems of prilocaine (PRL) and lidocaine (LID). In order to investigate the intermolecular interactions between water and co-amorphous PRL-LID systems, Fourier transform infrared spectroscopy (FTIR) and principal component analysis (PCA) were conducted. Water was found to bind with the carbonyl groups of PRL and LID molecularly evenly in the hydrated co-amorphous PRL-LID systems. Quantum chemical simulations visually confirmed the interactions between water and co-amorphous PRL-LID systems. Furthermore, the physical stability of hydrated co-amorphous PRL-LID systems was improved due to the anti-plasticizing effect of water, compared with the anhydrous samples. The preference of water to interact with the carbonyl groups of PRL and LID as binding sites could be associated with the anti-plasticizing effect of water on the co-amorphous PRL-LID systems.
KW - Anti-plasticizing
KW - Co-amorphous
KW - Effect of water
KW - Lidocaine
KW - Molecular interactions
KW - Prilocaine
U2 - 10.1016/j.ijpharm.2024.123807
DO - 10.1016/j.ijpharm.2024.123807
M3 - Journal article
C2 - 38220121
AN - SCOPUS:85183639849
VL - 651
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
M1 - 123807
ER -
ID: 382494964