Bromo and extraterminal domain (BET) inhibitors-
PROteolysis TArgeting Chimera (BETi-
PROTAC) is a new family of compounds that induce proteasomal degradation through the ubiquitination of the tagged to BET inhibitors Bromodomain
proteins, BRD2 and BRD. The encapsulation and controlled release of BET-
PROTACs through their vectorization with
antibodies, like
trastuzumab, could facilitate their pharmacokinetic and efficacy profile. Antibody conjugated nanoparticles (ACNPs) using
PROTACs have not been designed and evaluated. In this pioneer approach, the commercial MZ1
PROTAC was encapsulated into the FDA-approved polymeric nanoparticles. The nanoparticles were conjugated with
trastuzumab to guide the delivery of MZ1 to breast tumoral cells that overexpress HER2. These ACNPs were characterized by means of size, polydispersity index, and Z-potential. Morphology of the nanoparticles, along with stability and release studies, completed the characterization. MZ1-loaded ACNPs showed a significant cytotoxic effect maintaining its mechanism of action and improving its therapeutic properties.