: Existing cancer treatments are often accompanied by adverse side effects that can greatly reduce the quality of life of cancer patients; this sets the platform to the development and application of nanocarrier-based platforms for the delivery of anticancer drugs. Among these nanocarriers, liposomes have demonstrated excellent potential in drug delivery applications. Furthermore, the overexpression of certain receptors on cancer cells has led to the development of active targeting approaches where liposome surfaces are decorated with ligands against these receptors. Given the central role that sugars play in cancer biology, more and more researchers are integrating “glycoscience” into their anticancer therapeutic designs. Carbohydrate functionalized liposomes present an attractive drug delivery system due to their biocompatibility, biodegradability, low toxicity, and specific cell targeting ability. This review presents an overview of the preparation methods, characterization, evaluation, and applications of carbohydrate functionalized liposomes in cancer therapy.