ENZYME-RESPONSIVE NANOCARRIERS WITH TUNABLE RELESE RATES

Enzymes show great promise as triggers for disassembly of nanocarriers thanks to their over expression in diseased states tissue. Herein we show a highly modular design of amphiphilic linear-dendron hybrids block copolymers. These amphiphilic hybrids are composed of linear hydrophilic polyethyleneglycol (PEG) block and the hydrophobic block is an enzyme-responsive dendron with cleavable lipophilic chains as end-groups. These hybrids can spontaneously self-assemble into nano-size micelles that can disassemble and release its encapsulated cargo upon enzymatic hydrolysis of the hydrophobic end-groups. Taking advantage of this modular system, we show that small changes in the hydrophobic dendron building block can lead to dramatic changes of the assembled nanoparticle size and its rate of disassembly. This molecular study can potentially be applied to create smart drug delivery platform with tunable sizes and release rates.

References:

Rosenbaum, I.; Harnoy, A. J.; Tirosh, E.; Buzhor, M.; Segal, M.; Frid, L.; Shaharabani, R.; Avinery, R.; Beck, R.; Amir, R. J. "Encapsulation and Covalent Binding of Molecular Payload in Enzymatically Activated Micellar Nanocarriers" J. Am. Chem. Soc. 137, 6.