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| Content Provider | Royal Society of Chemistry (RSC) |
|---|---|
| Author | Shi, Liang Wei, Feng-Cai Pang, Bo Song, Xiao-Bin Liu, Ping Wang, Yong Wang, Ke-Tao |
| Copyright Year | 2016 |
| Abstract | In this study, docetaxel (DTX) was successfully conjugated to the monomethoxy-poly(ethylene glycol)-b-poly(lactide) (mPEG-PLA) polymer block via an ester linkage (DTX-PM). The polymer–drug conjugate resulted in the formation of nanosized micelles with a clear spherical shape. This size range is suitable for passive targeting via an EPR effect in cancer drug delivery. The DTX-PM exhibited a sustained release of the drug over 160 h with slightly accelerated release at acidic conditions. A cytotoxicity assay clearly revealed a time-dependent anticancer effect of DTX-PM in the squamous cancer cells. At 24 h incubation, the free drug exhibited a potent anticancer effect in the cancer cells while DTX-PM exhibited a superior anticancer effect by the end of 48 h incubation. The higher cytotoxic potential of DTX-PM suggests potential therapeutic advantages for cancer treatments. The annexin-V/PI based apoptosis assay further confirmed the anticancer potential of DTX-PM. The DTX-PM induced significantly higher cancer cell apoptosis in HSC-3 cancer cells. Importantly, DTX-PM significantly controlled the tumor progression in HSC-3 cancer cells bearing a tumor xenograft. Consistently, DTX-PM treated mice however showed a severe necrosis of the cancer cells in H&E staining and showed remarkably higher TUNEL positive apoptotic cells. Overall, a polymer–drug conjugate (DTX-PM) is a promising strategy to improve the therapeutic efficacy in oral squamous cell carcinoma. |
| Starting Page | 42819 |
| Ending Page | 42826 |
| Page Count | 8 |
| File Format | HTM / HTML PDF |
| ISSN | 20462069 |
| Volume Number | 6 |
| Issue Number | 49 |
| Journal | RSC Advances |
| DOI | 10.1039/c6ra03332f |
| Language | English |
| Publisher | Royal Society of Chemistry |
| Access Restriction | Open |
| Subject Keyword | Ethylene glycol HSC-3 Carcinoma Xenotransplantation Docetaxel Polymer Cytotoxicity Drug delivery Epithelium Lactide Necrosis Ester Cancer Apoptosis |
| Content Type | Text |
| Resource Type | Article |
| Subject | Chemistry Chemical Engineering |
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