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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Cyclodextrins as pharmaceutical solubilizers.

Cyclodextrins are cyclic oligosaccharide molecules of at least 6 subunits derived from starch, which form structures with lipophilic inner cavities and hydrophilic outer surfaces. Company Profile Email Us. 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 resulting in an increase in their apparent water solubility.


Modified Cyclodextrins are highly water-soluble themselves. I agree to the Terms and Privacy Statement.

Formulators have a powerful tool in the Cyclodextrin CD molecules; however there are several complicating factors that must be considered. The mechanism for this solubilization is rooted in the ability of cyclodextrin to form non-covalent dynamic inclusion complexes in solution.

A number of cyclodextrin-based products have reached the market based on their ability to camouflage undesirable physicochemical pharmaceuhical. 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.

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Get pharmacceutical latest articles from Outsourced Pharma delivered to your inbox. 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.


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. Company Name Velesco Pharmaceutical Services. For early toxicology studies, this is an added bonus to using CDs, but usually not a pivotal reason for their use.

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.

Substitutions are typically hydroxypropyl, although many other options are available.