A multifunctional
triblock copolymer intended for targeted drug
delivery applications has been designed and successfully synthesized.
Following various controlled polymerization and modification steps,
a saccharide end-functionalized polyoxyethylene block was attached
through an aromatic imine bond, cleavable in slightly acidic conditions,
to an amphiphilic diblock copolymer comprising a biodegradable
hydrophobic block and a partially modified with mitochondria targeting
ligands polycationic block. The micelles formed from the triblock
copolymer in aqueous media possess key functions (cleavable “stealth”
shield, targeting groups) needed for safe extracellular transport,
successful cell internalization, and drug delivery to the target cellular
organelles. The multifunctional nanocarriers were loaded with the
plant-derived anticancer drug curcumin, and in vitro analyses revealed that their cytotoxic, apoptogenic, and NF-κB-inhibitory
effects on target cells were superior over those of the free drug
and non-functionalized polymer micelles of similar composition. Moreover,
the enhanced cellular internalization and mitochondrial accumulation
of the multifunctional nanocarriers compared to their non-functionalized
analogues was visualized by fluorescence microscopy. The results indicate
that the presented multifunctional micelles have a potential for application
in nanomedicine for enhanced organelle-specific drug delivery.
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