Treatment modalities of various cancers and the delivery strategies of anticancer agents have evolved significantly in the recent past. The severity and fatality of the disease and hurdles to the effective delivery of therapeutic agents have drawn the attention of researchers across the world for proposing novel and effective drug delivery strategies for anticancer therapeutics. Attempts have been made to propose solutions to the diverse limitations like poor pharmacokinetics and higher systemic toxicities of the traditional delivery of anticancer agents. Nanotechnology-based drug delivery systems including lipid-based nanocarriers have demonstrated significant efficiency in this scenario. The review critically assessed the different types of lipid nanocarrier systems for the effective and optimal delivery of anticancer therapeutic agents. The diverse synthesis approaches are discussed for the laboratory scale and commercial development of different categories of lipid nanocarriers. Further, their application in anticancer drug delivery is illustrated in detail followed by a critical appraisal of their safety and toxicity.