The area of lipid molecular design is attracting widespread interest among numerous research groups worldwide. Diverse lipid assemblies in aqueous media, such as vesicles, bilayers and nanorods, offer new applications in chemical biology. Lipids with specifically tailored molecular architecture have been successfully employed as gene delivery vehicles, for controlled drug release and the preparation of supramolecular gels. Such molecular design of lipids, as well as their characterization upon membrane formation, offers an insight into the possible molecular basis of their properties. This in turn helps in the design of further generations of lipid systems with more predictable characteristics. Here, we present an overview of the current trends in lipid design and their utilization in various biochemical, physical and chemical applications.