Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocaine

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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.

Original languageEnglish
Article number123807
JournalInternational Journal of Pharmaceutics
Volume651
Number of pages7
ISSN0378-5173
DOIs
Publication statusPublished - 2024

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Publisher Copyright:
© 2024 The Author(s)

    Research areas

  • Anti-plasticizing, Co-amorphous, Effect of water, Lidocaine, Molecular interactions, Prilocaine

ID: 382494964