Self-Association of Cyclodextrins and Cyclodextrin Complexes

Cyclodextrins are useful functional excipients, which are being used in an ever-increasing way to camouflage undesirable pharmaceutical characteristics, especially poor aqueous solubility. It has generally been assumed that the mechanism whereby cyclodextrins exert their effects, especially their au...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2004-05, Vol.93 (5), p.1091-1099
Main Authors: Loftsson, Thorsteinn, Másson, Már, Brewster, Marcus E.
Format: Article
Language:English
Subjects:
aggregates
Biological and medical sciences
complexation
cyclodextrin
Cyclodextrins - chemistry
Cyclodextrins - pharmacokinetics
Drug Stability
General pharmacology
Medical sciences
non-inclusion
Permeability - drug effects
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
phase-solubility
self-association
Solubility - drug effects
solubilization
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Summary:Cyclodextrins are useful functional excipients, which are being used in an ever-increasing way to camouflage undesirable pharmaceutical characteristics, especially poor aqueous solubility. It has generally been assumed that the mechanism whereby cyclodextrins exert their effects, especially their augmentation of solubility, is via the formation of noncovalent, dynamic inclusion complexes. This is a model, which regards drug–cyclodextrin interactions as a discrete phenomenon and ignores the possible interaction of these complexes with one another. It is becoming increasingly apparent that such assumptions may not be universally applicable or all encompassing. Specifically, there is a growing body of evidence that supports the important contribution of non-inclusion-based aspects for drug solubilization by cyclodextrins including surfactant-like effects and molecular aggregation. This short review attempts to assess the available literature for areas in which such non-inclusion mechanisms are apparent and tries to interpret these in the context of a broader working theory as to how cyclodextrins exert their beneficial effects. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:1091–1099, 2004
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.20047