Nanocarriers have the utmost significance for advancements in drug delivery and nanomedicine technology. They are classified as polymer-based nanocarriers, lipid-based nanocarriers, viral nanoparticles, or inorganic nanoparticles, depending on their constituent parts. Lipid-based nanocarrier systems have gained tremendous attention over the years because of their noteworthy properties like high drug-loading capacity, lower toxicity, better bioavailability and biocompatibility, stability in the gastrointestinal tract, controlled release, simpler scale-up, and validation process. Nanocarriers still have some disadvantages like poor drug penetration, limited drug encapsulation, and poor targeting. These disadvantages can be overcome by their surface modification. Surface-modified nanocarriers result in controlled release, enhanced penetration efficiency, and targeted medication delivery. In this review, the authors summarize the numerous lipid-based nanocarriers and their functionalization through various surface modifiers such as polymers, ligands, surfactants, and fatty acids. Recent examples of newly developing surface-modified lipid-based nanocarrier systems from the available literature, along with their applications, have been compiled in this work.