Controlled PEGylation Crowdedness for Polymeric Micelles To Pursue Ligand-Specified Privileges as Nucleic Acid Delivery Vehicles.

A facile poly(ethylene glycol) (PEG) detachment scheme was utilized to control the PEGylation degree of the polymeric micelles. The performance of cyclic Arg-Gly-Asp (cRGD) as a targeted moiety was studied on a class of polymeric micelles with various PEGylation degrees, revealing that the specific cRGD-mediated cell affinity, thus the cellular uptake and implicated privileges including the ligand-specified favorable intracellular trafficking and consequent favorable biofunctions, was prominent for the polymeric micelles with high PEGylation degree. These results endow important information and implications for the design and development of targeted nanomedicine, particularly the delivery of vulnerable biological compounds.