Anti-tumor drug delivery system based on cyclodextrin-containing pH-responsive star polymer: in vitro and in vivo evaluation.

Int J Pharm

Tianjin Key Laboratory of Biomedical Materials, Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin 300192, PR China; Institute of Biomedical and Pharmaceutical Technology, Fuzhou University, Fuzhou 350002, PR China. Electronic address:

Published: October 2014

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A cyclodextrin-containing pH-responsive star polymer, with cyclodextrin polymer and pH-sensitive poly(2-(dimethylamino)ethyl methacrylate) as the core and poly(ethylene glycol) as the arm, was evaluated as drug carriers in vitro and in vivo. Doxorubicin (DOX) was successfully loaded into the star polymer to form nanoparticles (DOX-NPs) via host-guest interaction. The physicochemical properties such as drug loading content, size, morphology, stability and physical state of DOX-NPs were characterized in detail by (1)H NMR, DLS, SEM and DSC. Uniform and stable DOX-NPs with high encapsulation efficiency of 77.1% were obtained, and they also exhibited sustainable and controllable release of DOX in vitro. The cellular uptake of DOX-NPs was in concentration-, time- and cell type-dependent manners, and the cytotoxicity of DOX-NPs was significantly high toward HeLa and HepG2 cancer cells. Furthermore, in vivo anti-tumor experiment on BALB/c mice bearing cervical tumor showed that DOX-NPs could effectively suppress the growth of tumor without significant side effect. These findings suggest that the cyclodextrin-containing pH-responsive star polymer has a promising potential in developing novel drug delivery system for cancer therapy.

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http://dx.doi.org/10.1016/j.ijpharm.2014.08.018DOI Listing

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