화학공학소재연구정보센터
Journal of Colloid and Interface Science, Vol.514, 468-478, 2018
Stabilization of poly(ethylene glycol)-poly(epsilon-caprolactone) star block copolymer micelles via aromatic groups for improved drug delivery properties
Hypothesis: The functionalization of poly(ethylene glycol)-poly(epsilon-caprolactone) (PEG-PCL) block copolymers with moieties allowing for core-crosslinking is expected to result in improved micellar stability and drug delivery properties. Experiments: PEG-(PCL)(8) star block copolymers were functionalized with pendant benzylthioether (BTE) groups by applying an anionic post -polymerization modification technique followed by photoradical thiol-yne addition of benzyl mercaptan. The micellar properties of PEG-(PCL)(8) and PEG-(PCL-BTE)(8) were studied and compared in terms of critical micelle concentration (CMC), size, morphology, drug loading and release and in vitro cytotoxicity. Findings: In comparison with unmodified PEG-(PCL)(8) micelles, PEG-(PCL-BTE)(8) micelles exhibited a 15 fold lower CMC, a 15-fold smaller size and a 50% higher drug loading and encapsulation efficiency thanks to the presence of pendant benzyl groups which provide the possibility for micellar core-crosslinking via supramolecular pi-pi stacking and additional hydrophobic interactions. Whereas the PEG-(PCL)(8) micelles showed significant aggregation during in vitro cytotoxicity experiments, the PEG-(PCL-BTE)(8) micelles showed no signs of aggregation and were capable of solubilizing high concentrations of curcumin, resulting in a significant decrease in MCF-7 cell viability after 48 h. Their ease of synthesis combined with promising results regarding drug delivery make the PEG-(PCL-BTE)(8) micelles appealing for application in the field of encapsulation. (C) 2017 Elsevier Inc. All rights reserved.