Nano drug delivery system is the latest technology employed in various medicinal applications. This technology can be adapted to the conventional drug administration due to its site-specific targeting phenomena. The oral lipophilic drug administration has its drawbacks due to poor solubility and bioavailability. Lipid-based carrier systems are now widely popular due to improved efficiency, especially for lovastatin delivery. Lovastatin is an important drug which arrests the rate-limiting step of the cholesterol cascade. This drug has short half-lives, poor oral-administered bioavailability, poor solubility, and is rapidly metabolizable. Based on the composition, the drug delivery carriers are classified into solid lipid nanoparticles (SLNs), lipid emulsions (LEs), and nanostructured lipid carriers (NLCs). Among them, NLCs are a smarter generation of drug delivery carriers for lovastatin. The selection of various lipid systems and their formulation are discussed in this paper. Moreover, the characterization of these carrier systems to achieve the optimal characteristic features is discussed in a concise manner. © Seenivasan et al.