Background: Reaching the target cell has been the ultimate goal of nanoparticle-based drug delivery
because many drugs do not have the adequate physicochemical properties to reach or be taken up by target
cells. Therefore, site-specific drug delivery systems have been sought, aiming at overcoming many biological
barriers, thus improving drug performance.
Objective: Lipid nanoparticles emerged as a promising alternative for the usual colloidal drug carriers, prepared
with non-toxic solid physiological lipids and stabilized by common pharmaceutical surfactants. In addition
to the controlled or triggered release, solid lipid nanoparticles (SLN) can be designed to afford longer circulation
times improving the efficiency of drug delivery to the site of action. Over the past 20 years, several
passive or active functionalization approaches have been successfully applied to lipid nanoparticles intended
for targeting. A variety of ligands may be functionally SLN-attached including various internalizable ligands,
specific targeted peptides, saccharide ligands, or therapeutic molecules (e.g. antibodies or enzymes).
Conclusion: The present review focuses on the surface modification of lipid nanoparticles either SLN, nanostructured
lipid carriers (NLC), lipid drug conjugate nanoparticles (LDC) or lipid nanocapsules (LNC) with
specific molecules with the aim of improving its therapeutic and targeting performance.