Because of their bioadaptability and multi-functional characteristics, cycl
odextrins (CDs) are capable of alleviating the undesirable properties of dr
ug molecules in various routes of administration through the formation of i
nclusion complexes. This article outlines the current application of natura
l and chemically modified CDs in the design of advanced dosage forms. In an
oral drug delivery system (DDS), the hydrophilic and ionizable CDs can ser
ve as potent drug carriers in the immediate release- and delayed release-fo
rmulations respectively, while the release rate of water-soluble drugs can
be retarded by hydrophobic CDs. Since CDs are able to extend the function o
f pharmaceutical additives, the combination of molecular encapsulation with
other carrier materials will become effective and a valuable tool in the i
mprovement of drug formulation. Moreover, the most desirable attribute for
the drug carrier is its ability to deliver a drug to a targeted site; conju
gates of a drug with CDs can be a versatile means of constructing a new cla
ss of colon-targeting prodrugs. On the basis of this knowledge, the advanta
ges and limitations of CDs in DDS are addressed. (C) 1999 Elsevier Science
B.V. All rights reserved.