期刊
ASIAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 14, 期 1, 页码 78-85出版社
SHENYANG PHARMACEUTICAL UNIV
DOI: 10.1016/j.ajps.2018.03.002
关键词
Resveratrol; Docetaxel; Methoxyl poly(ethylene glycol)-poly(D,L-lactide) copolymer (mPEG-PDLA); Micelles; Drug resistance tumor
资金
- Liaoning Province Pan Deng Xue Zhe Grant
- Liaoning Provincial Education officer's Excellent Talents Supporting Plan
- National Natural Science Foundation of China [81302720, 81573380]
Co-delivery of anti-cancer drugs is promising to improve the efficacy of cancer treatment. This study was aiming to investigate the potential of concurrent delivery of resveratrol (RES) and docetaxel (DTX) via polymeric nanocarriers to treat breast cancer. To this end, methoxyl poly(ethylene glycol)-poly(D, L-lactide) copolymer (mPEG-PDLA) was prepared and characterized using FTIR and H-1 NMR, and their molecular weights were determined by GPC. Isobolo-gram analysis and combination index calculation were performed to find the optimal ratio between RES and DTX to against human breast adenocarcinoma cell line (MCF-7 cells). Subsequently, RES and DTX were loaded in the mPEG-PDLA micelles simultaneously, and the morphology, particle size distribution, in vitro release, pharmacokinetic profiles, as well as cytotoxicity to the MCF-7 cells were characterized. IC50 of RES and DTX in MCF-7 cells were determined to be 23.0 mu g/ml and 10.4 mu g/ml, respectively, while a lower IC50 of 4.8 mu g/ml of the combination of RES and DTX was obtained. The combination of RES and DTX at a ratio of 1:1 (w/w) generated stronger synergistic effect than other ratios in the MCF-7 cells. RES and DTX loaded mPEG-PDLA micelles exhibited prolonged release profiles, and enhanced cytotoxicity in vitro against MCF-7 cells. The AUC((0 -> t)) of DTX and RES in mPEG-PDLA micelles after i.v. administration to rats were 3.0-fold and 1.6-fold higher than that of i.v. injections of the individual drugs. These findings indicated that the co-delivery of RES and DTX using mPEG-PDLA micelles could have better treatment of tumors. (c) 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license. (http://creativecommons.org/licenses/by-nc-nd/4.0/)
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