Lipid‐based innovations have achieved new heights during the last few years as an essential component of drug development. The current challenge of drug delivery is liberation of drug agents at the right time in a safe and reproducible manner to a specific target site. A number of novel drug delivery systems has emerged encompassing various routes of administration, to achieve controlled and targeted drug delivery. Microparticulate lipoidal vesicular system represents a unique technology platform suitable for the oral and systemic administration of a wide variety of molecules with important therapeutic biological activities, including drugs, genes, and vaccine antigens. The success of liposomes as drug carriers has been reflected in a number of liposome‐based formulations, which are commercially available or are currently undergoing clinical trials. Also, novel lipid carrier‐mediated vesicular systems are originated. This paper has focused on the lipid‐based supramolecular vesicular carriers that are used in various drug delivery and drug targeting systems.