Cell targeting by a generic receptor-targeted polymer nanocontainer platform

Nanotechnology promises new avenues to medical diagnosis and treatment. Of special interest are injectable nanovehicles that are programmable towards specific targets, are able to evade the immune defense, and are versatile enough to be suited as carriers of complex functionality. Biotin-functionalized (poly(2-methyloxazoline)-b-poly(dimethylsiloxane)-b-poly(2-methyloxazoline) triblock copolymers were self-assembled to form nanocontainers, and biotinylated targeting ligands were attached by using streptavidin as a coupling agent. Specifically, fluorescence-labeled nanocontainers were targeted against the scavenger receptor A1 from macrophages, an important cell in human disease. In human and transgenic cell lines and in mixed cultures, receptor-specific binding of these generic carriers was followed by vesicular uptake. Low nonspecific binding supported the “stealth” properties of the carrier while cytotoxicity was absent. This versatile carrier appears promising for diagnostic or therapeutic medical use.