A simple method for the synthesis of porous polymeric vesicles and their application as MR contrast agents.

Because of their low membrane permeability the use of polymeric vesicles in certain drug delivery and molecular imaging applications and as bioreactors is less than ideal. Here, we report a simple method to prepare porous polymeric vesicles that possess high membrane permeability. Specifically, porous vesicles were produced from the aqueous assembly of the diblock copolymer PEG-PBD, and the triblock copolymer PEG-PPO-PEG. It was found that PEG-PPO-PEG-doped polymersomes exhibited improved membrane permeability to molecules less than 5 kDa. Further, these porous vesicles retained molecules ≥10 kDa within their aqueous interiors with no significant leakage. To demonstrate its application, highly efficient magnetic resonance contrast agents were produced from porous polymersomes by encapsulating macromolecules labeled with gadolinium. Due to a fast water exchange rate with surrounding bulk water, these paramagnetic porous polymersomes exhibited higher r1 relaxivity compared with Gd-encapsulated vesicles with no pores. Due to their simplicity, the porous polymersomes prepared with this method are expected to have additional useful applications.