Pharmaceutical Formulations

Cyclodextrins (CDs) are “cone-shaped” cyclic oligosaccharides, with a hydrophobic cavity and hydrophilic outer surface.

These nanoscale substances have long been used as functional excipients in different pharmaceuticals due to their ability to

encapsulate drugs and alter their disadvantageous features, e.g. increase the aqueous solubility, improve bioavailability, enhance

chemical stability or simply to mask their taste. At present more than 40, CD-enabled human pharmaceutical products are

on the market. The present of CDs is thus dominantly being used as excipients. The most favored are 2-hydroxypropyl-β-

CD (HPBCD) and sulfobutylether-β-CD, applied in dozens of parenteral formulations, while other derivatives are used for

oral, topical, nasal or ocular administration. The marvel of CDs lies in their flexibility: you can optimize the excipient for

the active ingredient and for the purpose simultaneously. In the present lecture illustrative drug products will be highlighted

demonstrating the applicability of derivatized oligosaccharides in the development of drug formulations. Outlook to the future

potential related to drug delivery use of CDs will also be provided. CDs tagged with biological recognition-based labeling were

prepared in order to deliver specific drugs to the site of action. Also, combinations with the application of colloidal structures

(dispersions, liquid crystals and macromolecules) will be discussed. Yet the future of CDs is not limited to being used as

excipients. We can harvest from their complex forming ability in vivo as well, in products, containing CDs as APIs. While the

initial idea was to use CDs as detoxification agents or to selectively remove chemicals from the system (e.g. Sugammadex –

Bridion), this concept has grown into clinical trials and studies using CDs as API alone (HPBCD as an orphan drug against

Niemann-Pick C, Focal Segmental Glomerulosclerosis or Alport Syndrome). A number of further therapeutic applications of

CDs themselves are expected to come, some potential areas will be reviewed.