Stable polymersomes with semipermeable membranes were prepared by simple mixing of two oppositely charged diblock copolymers containing zwitterionic and cationic (PMPC20-b-PMAPTAC(190)) or anionic (PMPC20-b-PAMPS(196)) blocks. The formation of vesicular structures in the mixed solution of the block copolymers was confirmed by direct observation using the cryo-TEM technique.
Superparamagnetic iron oxide nanoparticles coated with a cationic chitosan derivative (SPION/CCh) and decorated with a fluorescent probe molecule were next incorporated into the polymersome structure. The average diameter of SPION/CCh-polymersomes estimated using cryo-TEM was about 250 nm.
Surface topography of the SPION/CCh-loaded vesicles was imaged using AFM and the magnetic properties of these objects were confirmed by MFM and MRI measurements. The ability of SPION/CCh-polymersomes to affect T-2 relaxation time in MRI was evaluated based on the measurements of r(2) relaxivity.
The obtained value of r(2) (573 +/- 10 mM(-1) s(-1)) was quite high. The cytotoxicity and intracellular uptake of the SPION/CCh-loaded vesicles into EA. hy926 cells were studied.
The results indicate that the SPION/CCh-polymersomes seem to be internalized by vascular endothelium and are not cytotoxic to endothelial cells up to 1 mu g Fe per mL. Therefore, it can be suggested that SPION/CCh-polymersomes could prove useful as T-2 contrast agents in the MRI of endothelium.