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Novel methods in drug formulation

Drug development is a complex, laborious and time-consuming process that largely relies on empirical screening to control the drug crystal form. A European study developed a novel gel-based technology for controlling and studying the crystal structure of new drugs.
Novel methods in drug formulation
Drug development and formulation constitutes a great investment in modern societies and entails the empirical screening of drug substances to determine the range of polymorphic crystal forms available. Different crystal forms have different bioavailability and solubility, while crystal morphology significantly affects processing and tableting behaviour.

Before deciding on one form, the pharmaceutical industry identifies and investigates all polymorphic and solvate forms of new drug entities. This thorough characterisation of the solid-state chemistry of a new drug substance is also necessary from a regulatory standpoint. As a result, there is a great demand for novel, modern polymorph screening technologies. Recently, methods based on growing crystals from self-assembled fibres of low-molecular-weight gelators have emerged as alternatives to traditional gel media.

The scope of the EU-funded GELCRYS (A supramolecular gel control of pharmaceutical crystal growth) project was to explore the potential of supramolecular gels as a medium for crystal growth. The approach tested involved the chemical targeting of the gelator structure with functional groups to match that of the drug substance.

For this purpose, researchers prepared a series of cisplatin-mimetic metal complexes with urea functional groups that exhibited enhanced solubility in organic solvents and also formed fibrous networks. They investigated the capacity of these complexes to form gels in different solutions and used scanning electron microscopy to examine the morphologies of these gels. The insolubility of the drug cisplatin in organic solvents was addressed using a two-phase diffusing approach. The technique resulting in the discovery of a new N,N-dimethylacetamide solvate of the drug.

Overall, results indicate that the structural and geometrical resemblance between the cisplatin-mimetic gelator and the actual drug favours crystallisation. This appears to be the first evidence for the use of a drug-mimic supramolecular gel system that influences the outcome of a drug crystallisation process. Furthermore, it opens up the path for further research in this field, including other important drug molecules, and has tremendous valorisation potential in the pharmaceutical industry.

Related information


Drug, crystal structure, pharmaceutical, gelators, supramolecular, crystal growth, cisplatin
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