The utility of cyclodextrins in pharmaceutical dosage forms comes from the fact utility of cyclodextrins as efficient solubilizers depends on the. Brewster, M.E. and Loftsson, T. () Cyclodextrins as Pharmaceutical Solubilizers. Advanced Drug Delivery Reviews, 59, Considerations in using Cyclodextrins as solubilizers for early toxicology studies. Lisa Z. Crandall, MS. Early stage drug development can frequently be hindered.

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Company Profile Email Us. This review is intended to give a general background to the use of cyclodextrin as solubilizers as well as highlight kinetic and thermodynamic tools and parameters useful in the study of drug solubilization by cyclodextrins.

The mechanism for this solubilization is rooted in the ability of cyclodextrin to form non-covalent dynamic inclusion complexes in solution. Substitutions are typically hydroxypropyl, although many other options are available. This interaction and the exposure of the hydrophilic outer Cyclodextrin surface allow CD molecules to solubilize some poorly soluble lipophilic compounds.


Cyclodextrins are useful functional excipients that have enjoyed widespread attention and use. A number of cyclodextrin-based products have reached the market based on their ability to camouflage undesirable physicochemical properties. Formulators have a powerful tool in the Cyclodextrin CD pharmafeutical however there are several complicating factors that must be considered.

Cyclodextrins as pharmaceutical solubilizers.

The basis for this popularity from a pharmaceutical standpoint, is the ability of these materials to interact with poorly water-soluble drugs and drug candidates ccylodextrins in an increase in their apparent water solubility. Other solubilizing attribute may include the ability to form non-inclusion based complexes, the formation of aggregates and related domains and the ability of cyclodextrins to form and stabilize supersaturated drug solutions.

For early toxicology studies, this is an added bonus to using CDs, but usually not a pivotal reason for their use. Cyclodextrins are cyclic oligosaccharide molecules of at least 6 subunits derived pharmaecutical starch, which form structures with lipophilic inner cavities and hydrophilic outer surfaces.


Get the latest articles from Outsourced Pharma delivered to your inbox. Company Name Velesco Pharmaceutical Services.

Considerations In Using Cyclodextrins As Solubilizers For Early Toxicology Studies

Crandall, MS, Velesco Pharma Early stage drug development can frequently be hindered by compound solubility and the need to deliver large doses to animals with as little vehicle toxicity as possible. I agree to the Terms and Privacy Statement. Modified Cyclodextrins are highly water-soluble themselves.