Sugars including monosaccharides, oligosaccharides and polysaccharides are useful material in the approach of drug delivery system (DDS). In addition to these natural sugars, neoglycoproteins and neoglucoconjugates have been artificially developed. Diversity in their structures and functions provides a variety of possibilities to prepare DDS for drug targeting, control of gastrointestinal drug absorption and controlled release of drugs. In this article, these approaches will be briefly reviewed. © 2004, THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM. All rights reserved.