An antifouling macromolecular carrier can remarkablely increase the efficiency of drug and bioprobe delivery and reduce the systematic toxicity via decreasing the capture by the mononuclear phagocyte system (MPS) in liver and spleen. Herein, a facile synthesis of polyglycerol dendrimer (PGD) was developed by reducing synthesis steps and simplifying purification procedure through using β-CD as the core, and the PGD was modified with L-cysteine to produce a zwitterionic PGD, which showed strong antifouling property against protein adhesion and thus was able to escape from the capture by MPS in liver. The anti-fouling dendrimer was used to prepare antifouling dendritic MRI contrast agent (CA) by conjugation the zwitterionic PGD with DOTA-NHS and chelation with Gd<sup>3+</sup>. The in vivo MRI indicated that the antifouling dendritic CA had much higher and longer MRI contrast enhancement in blood pool than the clinically used CA (Magnevist) and minimal retention in liver.

Facile synthesis of antifouling dendrimer for drug and bioprobe delivery

249th National Meeting (2015)

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