Nanocarriers are effective non-viral vectors for drug and gene delivery with low immunogenicity in comparison with viral vectors. However, the lack of organ or cell specificity sometimes hinders their application and brings about unexpected side effects. Active targeting is an outstanding strategy recently developed for drug delivery systems, for example, surface modification of nanocarriers with specific ligands could target the pathological area to provide the maximum therapeutic efficacy. In such cases, the characteristics of the ligands determine the active targeting abilities of the nanocarrier systems. Recently, more attentions have been paid to saccharides as ligands for saccharidemodified nanocarriers, possesing the receptor-mediated targeting properties and showing the potential for cell-specific delivery of drugs and genes. In this review, various kinds of glycosylated nanocarriers are discussed, including: varying ligands, targeting properties, therapeutic effects, and methods for administering the nanocarriers. The advantages as well as the probable associated drawbacks of these vectors are communicated.