Though modern available cancer therapies are effective, they are connected with major, disagreeable adverse effects, causing non-compliance to patients. Furthermore, the majority of the polymeric-based medication platforms are certainly not universally acceptable, due to their several restrictions. With this juxtaposition, lipid-based medication delivery systems have appeared as promising drug nanocarriers to replace the majority of the polymer-based products because they are in a position to reverse polymer- as well as, drug-associated restrictions. Further, the amalgamation of the basic principle of nanotechnology in designing of lipid nanocarriers, which are the latest era of lipid carrier, having tremendous chemotherapeutic possibilities as tumor-targeted drug-delivery pertaining to tumor therapy. Apart from this, it is reported that nearly 40% of the modern medication entities are lipophilic. Further, research continues to be efficient to attain a significant understanding of the absorption and bioavailability of the developed lipids systems.