Captisol – Cyclodextrin

Captisol® is a patent protected, uniquely modified cyclodextrin, whose chemical structure was rationally designed to enable the creation of new products by significantly improving solubility, stability, bioavailability and dosing of active pharmaceutical ingredients (APIs).

Captisol 50% aqueousHow does Captisol work?

Traditional formulation systems for very insoluble and/or unstable active pharmaceutical ingredients (APIs) have involved a combination of organic solvents, surfactants and extreme pH conditions. These formulations may precipitate upon injection, or may cause irritation and adverse reactions. At times, these approaches are inadequate for solubilizing enough active agent for a preferred formulation.

Captisol® Solubilizes

Neutral, cationic and anionic APIs have been effectively associated with Captisol®. Aqueous solubilities have increased by a factor of 10 to 25,000, depending on the compound. In contrast to other solubilization technologies, product or traditional formulation system, the feasibility and solubility effectiveness of Captisol® can be rapidly assessed with a few simple lab experiments.

Captisol® Facilitates Delivery

Typically, the inherent pharmacokinetics and pharmacodynamics of the drug are unaffected by Captisol®, however onset may be manipulated and dose sparing maybe observed compared to classical formulations such as co-solvent based, emulsions or suspensions. Upon administration, Captisol® is readily and essentially completely renally eliminated. Captisol® formulations are biocompatible and can be administered parenterally, orally, ophthalmically, nasally, topically and via inhalation.

Ligand LogoCaptisol® is Safe

Captisol® was designed to maximize safety by eliminating the potentially damaging effects produced by the parent beta-cyclodextrin. In-vitro experiments and in-vivo acute, subchronic and chronic toxicity studies have provided safety data to support the development and approval of Captisol® drug formulations in man.

Captisol® Stabilizes

Interaction with Captisol® provides a beneficial and protected environment for the API in its lipophilic cavity, while Captisol’s hydrophilic surface provides excellent water solubility- boosting both solubility and stability. Interaction of the API with Captisol® can reduce decomposition by protecting labile regions from the potential reactants in the aqueous environment.


Captisol® Facilitates Faster Development

Using Captisol® early in the development process can increase the number of candidates that can be evaluated, decrease development time and increase lead candidate survivability. Captisol® enables an aqueous formulation for many water insoluble APIs as oral, nasal, topical, ophthalmic or liquid-presented medications.

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Captisol with water

Product Advantage

Product development is a complex process from discovery and evaluation through development and commercialization. Captisol® provides a useful and elegant solution to solubility and stability hurdles faced during each phase of the development process.

Combinatorial chemistry, high throughput screening (HTS) and molecular genetics have led to an increase in the number of insoluble and unstable molecules, peptides and proteins being investigated for their therapeutic activity.

Liquid Captisol AdThe Captisol® Advantage

  • Improved Stability
  • Allows formulation of water-insoluble APIs in all dosage forms, including oral, injectables, ophthalmic, nasal, topical and inhalation products


  • Tastelessness in oral formulas (taste masking in oral, nasal and Inhalation preperations)
  • Reduction of Irritation at site of injection in injectable formulas (parenteral)

Rapid Onset

  • Potential to enable faster acting versions of many currently approved oral products


  • cGMP manufacturing via a validated process
  • Multi-metric ton Commercial scale
  • Well-defined impurtiy profile and long term stability

Enables high Levels of API to reach dosing Targets

  • Improved Stability
  • Interaction with Captisol shelter the API from oxidative and hydrolytic degradation
  • Protects against effects from Elements such as heat and light

Improved Bioavailability and Delivery Efficiency

  • Better bioavailability than Methods of solubulization using nanoparticles and solvent systems
  • Permits lower dosing of APIs (i.e. potential for dose sparing)
  • Compatibility

Improved Safety, Compatibility and Convenience

  • Excellent safety record
  • Fist U.S. approved products in 2002
  • Simplified prepratation process, eliminating the Need for Refrigeration for some Commercial products

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Captisol, a Ligand technology

3911 Sorrento Valley Road

Suite 110

San Diego, CA 92121

Erika Luib

Marketing and Captisol Customer Service

P: 877-575-5593

Mail Captisol


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