title: Synergistic effect of PEGylated resveratrol on delivery of anticancer drugs.
abstract: Resveratrol (RES) is a natural polyphenol which can be considered as a nutraceutical because of its benefits such as anticancer and antioxidant activity. In this paper, we designed polymer-RES conjugates as anticancer drug carrier for synergistic therapeutic effect in cancer treatment. Bicalutamide (BIC) was used as a model drug to investigate the drug release behaviors and in vitro anticancer performance. PEG-RES and PEG-Glycine-RES nanoparticles were prepared and characterized. The size of the prepared particles was around 50 nm with RES content of 17.2 and 16.3 wt% for PEG-RES and PEG-Glycine-RES, respectively, and BIC loading efficiency were of 81.6% and 84.5%, separately. Release rate of RES from conjugates depended on the stability of ester group against hydrolysis. BIC release was much faster than RES release. The anticancer activity of BIC loaded PEGylated RES nanoparticles was much better than that of free BIC, indicating the conjugates provided a synergetic cytotoxicity to cancer cells. Confocal laser scanning microscopy observation and flow cytometry analyses indicated that PEGylated RES conjugates were more efficiently internalized into cells, released drug into cytoplasm. These results suggest that PEGylated RES conjugates show great potential for cancer therapy.
authors.affiliation: State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Wenlong
authors.initials: W
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Liang
authors.initials: L
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China. Electronic address: leyuan@mail.buct.edu.cn.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Le
authors.affiliation: State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China; Research Center of the Ministry of Education for High Gravity Engineering and Technology, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Jian-Feng
authors.initials: JF
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Jiexin
authors.initials: J
authors.lastname: Wang
authors.affiliation: School of Chemical Sciences & Engineering, University of New South Wales, Sydney NSW 2052, Australia.
authors.forename: Jimmy
authors.initials: J
authors.lastname: Yun
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004357:Drug Synergism; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D000077185:Resveratrol; D013267:Stilbenes / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013267:Stilbenes; D011092:Polyethylene Glycols; D000077185:Resveratrol
keywords: Anticancer; Conjugates; PEGylated RES; Synergistic effect