Journal
BIOMACROMOLECULES
Volume 12, Issue 10, Pages 3460-3468Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bm200956u
Keywords
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Funding
- National Natural Science Foundation of China [20974062]
- National Basic Research Program [2009CB930400]
- Shanghai Leading Academic Discipline Project [B202]
- China National Funds for Distinguished Young Scientists [21025417]
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Oxime bonds dispersed in the backbones of the synthetic polymers, while young in the current spectrum of the biomedical application, are rapidly extending into their own niche. In the present work, oxime linkages were confirmed to be a robust tool for the design of pH-sensitive polymeric drug delivery systems. The triblock copolymer (PEG-OPCL-PEG) consisting of hydrophilic poly(ethylene glycol) (PEG) and hydrophobic oxime-tethered polycaprolactone (OPCL) was successfully prepared by aminooxy terminals of OPCL ligating with aldehyde-terminated PEG (PEG-CHO). Owing to its amphiphilic architecture, PEG-OPCL-PEG self-assembled into the micelles in aqueous media validated by the measurement of critical micelle concentration (CMC). The MTT assay showed that PEG OPCL PEG exhibited low cytotoxicity against NIH/3T3 normal cells. Doxorubicin (DOX) as a model drug was encapsulated into the PEG-OPCL-PEG micelles. Drug release study revealed that the DOX release from micelles was significantly accelerated at mildly acid pH of 5.0 compared to physiological pH of 7.4, suggesting the pH-responsive feature Of the drug delivery systems with oxime linkages. Flow cytometry and confocal laser scanning microscopy (CLSM) measurements indicated that these DOX-loaded micelles were, easily internalized by living cells. MTT assay against HeLa cancer cells showed DOX-loaded a high anticancer efficacy. All of these results demonstrate that these polymeric micelles self-assembled from oxime-tethered block copolymers are promising carriers for the pH-triggered intracellular delivery of hydrophobic anticancer drugs.
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