Liposomes are one of the most successfully targeted drug delivery systems and are attracting increasing attention in the biomedical field due to their excellent properties such as potent payload ability for both hydrophobic and hydrophilic active agents and biopharmaceuticals, biocompatibility, and scalability. To date, over 21 liposomal formulations have been approved for clinical use, and approximately 28 liposomal products are under clinical trial. In this chapter, we will discuss the use of liposomes in targeted drug delivery based on the classification of composition.