This article reviews the potential of polyrotaxanes in drug delivery with t
he historical background of polyrotaxane syntheses. Pseudopolyrotaxanes and
polyrotaxanes, including classifications, synthetic methods, structures an
d physical properties are discussed in the first section. The second sectio
n provides our concept of drug carriers using drug-polyrotaxane conjugates
in comparison with conventional drug-polymer conjugates. The third and four
th sections describe the synthetic method for biodegradable polyrotaxanes,
the conjugation with drugs, and their association under physiological condi
tions. The fifth section discusses other possibilities for the polyrotaxane
s such as drug penetration enhancers. These studies suggest the potential o
f polyrotaxanes in pharmaceutical applications.