Stabilization of poly(ethylene glycol)-poly(ε-caprolactone) star block copolymer micelles via aromatic groups for improved drug delivery properties

JOURNAL OF COLLOID AND INTERFACE SCIENCE

卷:514

Article

Buwalda, Sytze¹  Al Samad, Assala^1,2  El Jundi, Ayman^1,2  Bethry, Audrey¹  Bakkour, Youssef²  Coudane, Jean¹  Nottelet, Benjamin¹ 

[1] Univ Montpellier, CNRS, ENSCM, IBMM,UMR5247, Montpellier, France

[2] Lebanese Univ, Fac Sci 3, Lab Appl Chem, POB 826, Tripoli, Lebanon

关键词: Poly(ethylene glycol)poly(epsilon-caprolactone);    Stabilized micelle;    Controlled drug delivery;    Supramolecular assembly;   

DOI  :  10.1016/j.jcis.2017.12.057

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

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