This volume describes the protocols for fabrication of liposomal drug delivery system, and consists of two parts. The first part emphasizes the basic protocols and concepts for fabrication of drug-loaded liposomes. For new investigators, laying the groundwork is the first step. This part focuses on the fabrication details in liposomes formulations, which are the so-called small tricks while usually not disclosed in mostly published research articles. However, these processing details are crucial for the preparation of liposomes. And the second part focuses on the strategies in modified and/or functionalized liposomes to adapt to pathophysiological environment, as well as their application in treating diseases. As new analytical and synthetic technologies become available, and improved understanding of pathophysiology, various functionalized drug liposomes are developing to fit the requirements of different therapeutic purposes, exhibiting a broad range of applications. Accordingly, the objectives of this part are aimed at deeply unearthing the formulation of drug-loaded liposomes, describing the detailed operation of liposomal formulation, and further demonstrating their potential applications. Therefore, this volume shows the features of experimental report or protocol for proving a guide to scientists, research students, and young investigators in pharmaceutical enterprises.