PDCs

Phospholipid drug conjugate (PDC), also known as phospholipid-based prodrug, refers to a newly important class of therapeutic agents or pro-drugs, formed by one or more pharmaceutical molecules covalently bound to a specific phospholipid, which is a kind of bioreversible derivatives of active drug molecules with the potential to improve some physiological barriers. The PDC approach is mainly associated with targeting the phospholipase A₂ enzyme, which specifically hydrolyzes the sn-2 fatty acyl bond of phospholipid with arachidonic acid and lysophosphatidic acid release. The design of the drug moiety covalently attached to the sn-2 position of a phosphate group is proposed to avoid the hydrolysis, thereby enabling the PDCs to be absorbed into the metabolic phospholipid processing pathways.

PDCs have received much attention in the past few decades and have been widely studied and applied as new targeted therapies, mainly due to their outstanding advantages and ease of synthesis and production. Compared with other lipid-based drug delivery systems like liposomes, lipid particulate, and lipid-core micelles, PDCs are more flexible in structure with higher drug loading, specificity, and permeability, which show the potential to develop promising and targeting therapeutic agents in clinics.