Nanocrystallization of Rare Tolbutamide Form V in Mesoporous MCM-41 Silica

Nartowski, Karol, Malhotra, Diksha, Hawarden, Lucy, Fabian, Laszlo and Khimyak, Yaroslav (2018) Nanocrystallization of Rare Tolbutamide Form V in Mesoporous MCM-41 Silica. Molecular Pharmaceutics, 15 (11). 4926–4932. ISSN 1543-8384

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    Encapsulation of pharmaceuticals inside nanoporous materials is of increasing interest due to their possible applications as new generation therapeutics, theranostic platforms, or smart devices. Mesoporous silicas are leading materials to be used as nanohosts for pharmaceuticals. Further development of new generation of nanoscale therapeutics requires complete understanding of the complex host−guest interactions of organic molecules confined in nanosized chambers at different length scales. In this context, we present results showing control over formation and phase transition of nanosize crystals of model flexible pharmaceutical molecule tolbutamide confined inside 3.2 nm pores of the MCM-41 host. Using low loading levels (up to 30 wt %), we were able to stabilize the drug in highly dynamic amorphous/disordered state or direct the crystallization of the drug into highly metastable nanocrystalline form V of tolbutamide (at loading levels of 40 and 50 wt %), providing first experimental evidence for crystallization of pharmaceuticals inside the pores as narrow as 3.2 nm.

    Item Type: Article
    Uncontrolled Keywords: drug delivery,encapsulation,mesoporous silica,polymorphism,solid-state nmr,tolbutamide
    Faculty \ School: Faculty of Science > School of Pharmacy
    Depositing User: LivePure Connector
    Date Deposited: 03 Oct 2018 16:30
    Last Modified: 09 Apr 2019 13:47
    DOI: 10.1021/acs.molpharmaceut.8b00575

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