Fluorescence-Labeled Immunomicelles: Preparation, in vivo Biodistribution, and Ability to Cross the Blood-Brain Barrier

Multifunctional hybrid micelles are prepared from amphiphilic mal-PEG-b-PLA and mPEG-b-P(LA-co-DHC/RhB) block copolymers. A specific anti-transferrin receptor antibody, OX26, is linked onto the surface of the micelles. ELISA indicates that the conjugated antibody preserves its activity. OX26 conjugation can increase the uptake efficiency of micelles by target cell lines (C6). Pharmacokinetics and in vivo biodistribution experiments are carried out to investigate the ability of OX26-conjugated micelles (immunomicelles) to cross the bloodbrain barrier. The data show that the brain uptake of OX26-conjugated micelles is much more than that of OX26-free ones. Therefore, OX26-conjugated micelles will be promising drug carriers to cross the blood-brain barrier.