Cyclodextrins as Early Stage Toxicology Formulation Solubilizers: These Things are Really Cool.

Cyclodextrins are powerful tools in the early stage formulator’s toolbox, especially with the poorly soluble compounds that we are frequently formulating.  Many of our clients are unfamiliar with these compounds, their limitations, and how they can be used for formulation.  One large advantage is that Cyclodextrins are typically water soluble, and therefore your formulation can be appropriate for IV and oral administration.

I recently wrote a white paper on this topic.  You can access it HERE.

In a nutshell, Cyclodextrins are “bucket shaped” cyclic oligosaccharide molecules based on 6 to 8 glucose molecules.  The more glucose molecules incorporated in the ring, the larger the inner diameter of the “bucket”.  Hydrophobic molecules can fit into the “bucket” and be shielded from the aqueous media.  There are a variety of Cyclodextrins available with different modifications.

Co-solvents like NMP (n-methylpyrrolidone) can sometimes be used with Cyclodextrins to improve drug solubility for early non clinical studies.  This strategy has been quite successful for us in increasing drug loading for certain, appropriate toxicology studies.

Contact Velesco if you’d like to learn how we can help formulate your compound!

Fun fact: The active ingredient in some Febreze fabric spray is hydroxypropyl-β-cyclodextrin!

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