Critical Reviews™ in Therapeutic Drug Carrier Systems, 28(3), 255–292 (2011) 0743-4863/11/$35.00 ©2011 Begell House, Inc. www.begellhouse.com 255 Carbohydrate Molecules: An Expanding Ho rizo n in Drug De live ry a nd Bio m e d ic ine Raj Kumar Shukla 1* & Akanksha Tiwari 2 1 Sun Pharma Industries Ltd., Sun Pharma Advance Research Centre, Tandalja-390020. Bar- oda-Gujrat India; 2 Department of Pharmaceutics, Baroda College of Pharmacy, Parul Trust, Limbda, Waghodia-391760, Baroda- Gujrat *Address all correspondence to Rajkumar Shukla, Sun Pharma Industries Ltd., Sun Pharma Advance Research Centre, Tandalja-390020, Baroda-Gujrat India; Tel.: +91-9725515969; Fax: +91-265-2354897; rajrgpv@gmail.com ABSTRACT: This review presents successful applications of carbohydrate molecules in drug delivery, vaccine development, cancer, HIV and various other diseases based on advances in glycobiology and glycochemistry. Carbohydrate-mediated delivery could be site specific/cell specific. Carbohydrate-based delivery system has been successfully utilized for the delivery of macromolecular drugs, antigen, and potential therapeutic drug candidates. Lectin, the high affinity carbohydrate-binding nonimmune glycoproteins has specific and noncovalent binding sites for defined carbohydrates. Endogenous surface lectins of cancer cells participate in the regulation of tumor cell growth. The oligosaccharides constitute potential recognition sites for carbohydrate-mediated interactions between cells and drug carriers bearing suitable site directing molecules. The recognition of carbohydrate immunodeterminants has created great attention in the development of carbohydrate-based vaccines. Peptide mimotopes provide a strategy to augment human immunodeficiency virus 1 (HIV-1) specific carbohydrate reactive immune responses. Experimental cancer and HIV vaccines are being developed in attempts to overcome weak immunological responses to carbohydrate-rich surface antigens using carriers, adjuvants, and novel carbohydrate antigen constructs. Current carbohydrate-based vaccines are used for prostate cancer, typhus, pneumonia, and meningitis; vaccines for malaria, anthrax, and leishmaniasis are under development. This article discusses the current research involved in the role of carbohydrate molecules in targeted controlled drug delivery, immunology, and vaccine development. KEY WORDS: carbohydrate molecules, cell specific delivery, targeted drug delivery, im- munology, vaccines I. INTRO DUC TIO N Carbohydrates are simple sugars having the empirical formula C n H 2n O n , where n is Z3, suggesting that carbon atoms are in some way combined with water. They are also called “hydrates of carbon.” Glucose is a common monosaccharide that, after oxidation, forms carbon dioxide and water, providing energy source. The molecules of glucose may link together to form a variety of other macromolecules. In comparison to dipeptide consist- ing of amino acid that can produce single dipeptide, the glucose molecules can give rise to 11 different disaccharides. If we move to large scale, 24 tetrapeptides can be produced by 4 different amino acids; on the other hand, 4 different hexose monosaccharide may potentially produce 35,560 unique tetrasaccharides. 1