Amphiphilic Scorpion-like Macromolecules as Micellar Nanocarriers

Amphiphilic scorpion-like macromolecules (AScMs), that self-assemble as nanocarriers, were evaluated for intracellular delivery. To qualitatively examine the intracellular fate of AScMs in human umbilical vein endothelial cells (HUVECs), representative polymers (M ₁₂ P ₅ ) were labeled with a fluorescent dye, fluorescein isothiocyanate (FITC). The FITC-labeled M ₁₂ P ₅ micelles were prepared by mixing a low concentration of FITC-labeled M ₁₂ P ₅ polymer (10wt%) with unlabeled M ₁₂ P ₅ polymer (90wt%). Optical sectioning by confocal laser scanning microscopy of HUVECs incubated with FITC-labeled polymer micelles revealed that the polymers were localized in subcellular components within 60 min. Transmission electron microscopy was used to highlight the rapid accumulation of a polymer-encapsulated agent in the nucleus by 60 min. This study demonstrated that the M ₁₂ P ₅ polymers were internalized into HUVECs. Based on these data, the polymeric nanocarriers are potential candidates for intracytoplasmic and nuclear delivery of drugs, proteins and/or genes.