Surface engineering of nanomaterials with phospholipid-polyethylene glycol-derived functional conjugates for molecular imaging and targeted therapy

In recent years, phospholipid-polyethylene glycol-derived functional conjugates have been widely employed to decorate different nanomaterials, due to their excellent biocompatibility, long blood circulation characteristics, and specific targeting capability. Numerous in vivo studies have demonstrated that nanomedicines peripherally engineered with phospholipid-polyethylene glycol-derived functional conjugates show significantly increased selective and efficient internalization by target cells/tissues. Targeting moieties including small-molecule ligands, peptides, proteins, and antibodies are generally conjugated onto PEGylated phospholipids to decorate liposomes, micelles, hybrid nanoparticles, nanocomplexes, and nanoemulsions for targeted delivery of diagnostic and therapeutic agents to diseased sites. In this review, the synthesis methods of phospholipid-polyethylene glycol-derived functional conjugates, biophysicochemical properties of nanomedicines decorated with these conjugates, factors dominating their targeting efficiency, as well as their applications for in vivo molecular imaging and targeted therapy were summarized and discussed.