IPEC e-newsletter - Excipients Insight June/July 2017 - 10-07-17


Inside this issue


Excipients 'have potential as imaging agents'

Excipients are generally considered pharmacologically and toxicologically inactive, which allows them to be used at the levels needed in drug formulations without affecting the active ingredient. However, some have properties that could make them interesting contrast agents for use with medical imaging techniques, for example to image tumours in high detail, according to researchers in Italy.

The team are focusing on magnetic resonance imaging (MRI), which has become a go-to tool for healthcare, and in particular a variant called chemical exchange saturation transfer (CEST) that makes use of contrast agents to enhance the diagnostic power of the technology.

They have investigated the MRI-CEST properties of several excipients - ascorbic acid, sucrose, N-acetyl-d-glucosamine, meglumine and 2-pyrrolidone - and tested them as tumour-detecting agents in two animal models. They found a moderate to marked increase in CEST contrast with all the excipients, with meglumine and ascorbic acid performing the best, and suggest that these are superior to glucose - which has already been investigated for this application - as they reside within tumour cells for longer.

The excipients "show remarkable MRI-CEST properties as demonstrated by the in vivo visualization of tumours in two murine models," conclude the authors. "The extremely good safety profile of the excipients provides support to the view that these molecules may be considered reliable candidates for clinical translation."

The research is published in the International Journal of Pharmaceutics.




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