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

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    Accepted author manuscript, 1 MB, PDF-document

    Embargo ends: 24/09/19

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Abstract

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.

Details

Original languageEnglish
Pages (from-to)4926–4932
JournalMolecular Pharmaceutics
Volume15
Issue number11
Early online date24 Sep 2018
DOIs
StatePublished - 5 Nov 2018
Peer-reviewedYes

Keywords

    Research areas

  • drug delivery, encapsulation, mesoporous silica, polymorphism, solid-state NMR, tolbutamide

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