This article reviews our concept of drug delivery system using drug/polyrot
axane conjugates ns a drug carrier. The biodegradable polyrotaxanes exhibit
their supramolecular architectures: many cyclodextrins are threaded onto a
single poly(ethylene glycol) chain capped with biodegradable bulky endgrou
ps. The synthetic method of the polyrotaxanes, the conjugation with drugs,
and their association nature in a physiological condition are described. Th
e supramolecular dissociation of the drug/polyrotaxane conjugates via termi
nal peptide cleavage by a hydrolytic enzyme is discussed in relation to the
ir association nature. Through these studies, advantages of drug/polyrotaxa
ne conjugates as a drug carrier are suggested in comparison with convention
al drug/polymer conjugates.