Targeting Regulation of Dually Modified Liposomes by Polyethylene Glycol Length of Vesicle Surface

With aging of population, changing of living habits, and intake of high-fat diet, more and more people have been suffering from cardio-cerebral apoplexy. The synchronous treatment of cardio-cerebral conditions based on an integral strategy may bring benefit to the better clinical efficacy. The simultaneously-targeting delivery of active molecules by nanoscale carriers to heart and brain remains unmet problem. The physiological difference of targets between heart and brain makes it a huge challenge which one targeting ligand modification acquires the delivery of two organs and treatment, simultaneously. Traditionally, dually targeting strategies are introduced to enhance the selectivity for one aimed tissue and delivery efficiency of these particles. However, the interference between two targeting ligands on the surface of nanoscale carriers may influence the affinity of these ligands with their receptors or transporters, resulting to the change distribution of carriers. Herein, we observed that how anti-cardiac troponin I (cTnI) antibody (Ab) conjugated with the linker, polyethylene glycol (PEG), on the surface of liposomes influenced the affinity of mannose derivatives with transporter and regulated distribution of these vesicles in the heart and brain. The dually targeting liposomes can target to the heart and brain tissue simultaneously by the regulation length of PEG chain linking with p -pentanoic acid phenyl-α-D-acetylmannosamine (Ac₄MAN). These results may bring benefit to design the multi-modification of nanocarriers and the treatment of cardio-cerebral diseases.