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Novel Free-Paclitaxel-Loaded Redox-Responsive Nanoparticles Based on a Disulfide-Linked Poly(ethylene glycol)-Drug Conjugate for Intracellular Drug Delivery: Synthesis, Characterization, and Antitumor Activity in Vitro and in Vivo
Chuan, Xingxing; Song, Qin; Lin, Jialiang; Chen, Xianhui; Zhang, Hua; Dai, Wenbing; He, Bing; Wang, Xueqing; Zhang, Qiang
关键词Redox-response Paclitaxel Polymer-drug Conjugates/prodrugs Polymeric Nanoparticles Programmed Drug Release
刊名MOLECULAR PHARMACEUTICS
2014-10-01
DOI10.1021/mp500399j
11期:10页:3656-3670
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]CREMOPHOR-FREE ; MULTIDRUG-RESISTANCE ; POLYMERIC MICELLES ; GLUTATHIONE LEVELS ; TARGETED DELIVERY ; ANTICANCER DRUG ; GENE DELIVERY ; PHASE-II ; CANCER ; EFFICACY
英文摘要

To address the obstacles facing cancer chemotherapeutics, including toxicity, side effects, water insolubility, and lack of tumor selectivity, a novel stimuli-responsive drug-delivery system was developed based on paclitaxel-loaded poly(ethylene glycol)-disulfide-paclitaxel conjugate nanoparticles (PEG-SS-PTX/PTX NPs). The formulation emphasizes several benefits, including polymer-drug conjugates/prodrugs, self-assembled NPs, high drug content, redox responsiveness, and programmed drug release. The PTX-loaded, self-assembled NPs, with a uniform size of 103 nm, characterized by DLS, TEM, XRD, DSC, and H-1 NMR, exhibited excellent drug-loading capacity (15.7%) and entrapment efficiency (93.3%). PEG-SS-PTX/PTX NPs were relatively stable under normal conditions but disassembled quickly under reductive conditions, as indicated by their triggered-aggregation phenomena and drug-release profile in the presence of dithiothreitol (DTT), a reducing agent. Additionally, by taking advantage of the difference in the drug-release rates between physically loaded and chemically conjugated drugs, a programmed drug-release phenomenon was observed, which was attributed to a higher concentration and longer action time of the drugs. The influence of PEG-SS-PTX/PTX NPs on in vitro cytotoxicity, cell cycle progression, and cellular apoptosis was determined in the MCF-7 cell line, and the NPs demonstrated a superior anti-proliferative activity associated with PTX-induced cell cycle arrest in G2/M phase and apoptosis compared to their nonresponsive counterparts. Moreover, the redox-responsive NPs were more efficacious than both free PTX and the non-redox-responsive formulation at equivalent doses of PTX in a breast cancer xenograft mouse model. This redox-responsive PTX drug delivery system is promising and can be explored for use in effective intracellular drug delivery.

语种英语
WOS记录号WOS:000342857000043
项目编号81130059 ; 81273456
资助机构National Natural Science Foundation of China
引用统计
被引频次:41[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/51816
专题北京大学药学院_药剂学系
北京大学基础医学院
北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Chuan, Xingxing,Song, Qin,Lin, Jialiang,et al. Novel Free-Paclitaxel-Loaded Redox-Responsive Nanoparticles Based on a Disulfide-Linked Poly(ethylene glycol)-Drug Conjugate for Intracellular Drug Delivery: Synthesis, Characterization, and Antitumor Activity in Vitro and in Vivo[J]. MOLECULAR PHARMACEUTICS,2014,11(10):3656-3670.
APA Chuan, Xingxing.,Song, Qin.,Lin, Jialiang.,Chen, Xianhui.,Zhang, Hua.,...&Zhang, Qiang.(2014).Novel Free-Paclitaxel-Loaded Redox-Responsive Nanoparticles Based on a Disulfide-Linked Poly(ethylene glycol)-Drug Conjugate for Intracellular Drug Delivery: Synthesis, Characterization, and Antitumor Activity in Vitro and in Vivo.MOLECULAR PHARMACEUTICS,11(10),3656-3670.
MLA Chuan, Xingxing,et al."Novel Free-Paclitaxel-Loaded Redox-Responsive Nanoparticles Based on a Disulfide-Linked Poly(ethylene glycol)-Drug Conjugate for Intracellular Drug Delivery: Synthesis, Characterization, and Antitumor Activity in Vitro and in Vivo".MOLECULAR PHARMACEUTICS 11.10(2014):3656-3670.
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