Surface-Functionalized Lipid Nanoparticles for Site-Specific Drug Delivery

Abstract

Nanoparticles have been sought as drug carriers to increase bioavailability at the target site of action, improving drug therapeutic index. Among the several nanoparticulate systems proposed in the field of pharmaceutical technology, lipid-based nanoparticles (NPs) have attracted increasing attention due to their unique size-dependent properties, use of common well-tolerated, pharmaceutically accepted excipients, thus allowing for developing new delivery systems that could hold great promise for attaining the bioavailability enhancement along with controlled and site specific drug delivery. In the last years, passive and active modification approaches have been proposed to surface functionalization of lipid NPs intended for specific targeting. Internalizable ligands, specific targeted peptides, saccharide ligands, or even therapeutic molecules (e.g. antibodies or enzymes) are used for this purpose. Physicochemical properties of NPs can also be adjusted to improve drug targeting. The present chapter describes the recent advances in surface functionalization of lipid NPs, either solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), lipid–drug conjugate nanoparticles (LDC), or lipid nanocapsules (LNC) with specific ligands to enhance drug targeting performance as well as its therapeutic effect.