Facile Construction of Multifunctional Nanocarriers Using Sequential Click Chemistry for Applications in Biology

Bi- and trifunctional dendrimer and miktoarm nanocarriers, containing a combination of covalently linked model drug (α-lipoic acid), fluorescent dye (BODIPY), and poly(ethylene glycol) (PEG), are synthesized using a core with orthogonal functional groups, on which Huisgen alkyne−azide “click” reactions are performed in sequence. These carriers are internalized into the cells where they reduce H 2 O 2 induced reactive oxygen species formation. In addition, miktoarm nanocarriers conjugated with α-lipoic acid enhance intracellular glutathione (GSH) concentrations.