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.

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Carbohydrates have several unique biofunctions that are useful for drug delivery systems. To utilize these functions, glyco-conjugate design and chemistry are important. Glyco-conjugate materials consisting of polymeric materials and polysaccharides for DDS were described.

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Glucose concentration in circulating blood has to be strictly regulated to maintain the homeostasis in the body. Glucose transporters such as GLUT and SGLT families are believed to play important roles to control such blood glucose level, not only just by the transport of their substrates across plasma membranes, but also by the translocation of transporter proteins themselves as well as signal transduction as glucose sensors. In this review the intracellular trafficking of glucose transporters and molecular mechanism involved in such trafficking are summarized. The intracellular trafficking of asialoglycoprotein receptor, which is one of the promising targets for the drug delivery to hepatocytes, was also briefly reviewed.

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We designed a novel artificial extracellular matrix that mimics an extracellular matrix in organisms. Covalently crosslinked gel of heparin and alginate showed binding and slow release of bFGF, a representative member of the heparin-binding growth factors, as well as VEGF and HGF. Since these released growth factors showed marked biological activities both in vitro and in vivo, it is hoped to treat ischemic diseases and repair of injured liver, kidney, skin, and nerve.

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Carbohydrate molecules such as glycoprotein, glycolipid, and proteoglycan being expressed on cell surface alter during carcinogenesis but also play important roles in cancer invasion and metastasis. Here, we reviewed the recent advances in glycobiology for cancer treatment. Cancer treatment utilizing glycobiology techniques is categorized as 1) inhibition of carbohydrate chain synthesis, 2) inhibition of lectin which specifically reacts with a carbohydrate structure, 3) activation of innate immunity, 4) antibody drugs raised against carbohydrate chain, and 5) cancer vaccines. Some of these techniques have been approved by the U.S. Food and Drug Administration. Several companies and academic institutions are conducting clinical trials of carbohydrate based anti-cancer drugs, which could be a promising approach because of its minimal side effect.

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