Captisol® in Formulations

How does Captisol® improve formulations?

Captisol® is a modified cyclodextrin that can form ionic and inclusion complexes with many types of drugs. Complexation can significantly increase the solubility and often times, the physico chemical stability of the drug. Complexation has also been used to improve dissolution and bioavailability, reduce volatility, allow incorporation of liquids into solid formulations, and reduce unpleasant side effects such as taste and irritation caused by drug contact with tissues, e.g. extravasation at injection sites and GI irritation. 

Will Captisol® complex with my drug candidate?

In general, Captisol® will complex with many hydrophobic compounds that have structural features that can fit within the cyclodextrin cavity. A significant amount of literature is available illustrating the types of compounds that are candidates for inclusion complexation, but confirmation must be made by conducting a few simple laboratory tests. 

Will Captisol® complex with peptides and proteins?

Complexation can occur between Captisol® and peptides/proteins through the side chains of individual amino acids. The complexation can assist in solubilization, stabilization, particularly in terms of reduced aggregation, and refolding, which can lead to improved bioavailability. Cyclodextrins can also improve the effectiveness of antisense therapies by assisting in:

  • Cellular uptake (Zhao, et. al. 1995; Abdou, et. al.)
  • Internalization (Croyle, et. al.)
  • Nuclease resistance of oligonucleotides (Habus, et. al.)
  • Improved activity (Abdou, et. al.)
  • Reduced side effects (Zhao et. al. 1996) 

Can Captisol® be used in injectable formulations?

Yes. An extensive toxicology package has been developed demonstrating the safe use of Captisol® for parenteral administration (intravenous, intramuscular and subcutaneous). This information can be made available for client review upon request. 

Can Captisol® be given by non-parenteral routes?

Safety studies have been conducted with Captisol® for many different routes of administration, including oral, ophthalmic, inhalation and nasal. CyDex has completed numerous safety studies in rat, mice, dog, rabbit and monkey by these different routes of administration. Final reports have been submitted to the FDA in our Type V DMF and are available to clients under applicable agreements. 

Is Captisol® suitable for use in solid formulations?

Captisol® has been used quite successfully in solid formulations to assist in solubilization, dissolution and improved absorption. 

How to Use Captisol®

View our easy-to-use PDF for more information on how to use Captisol®

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