学科主题药学
The effect of linkers on the self-assembling and anti-tumor efficacy of disulfide-linked doxorubicin drug-drug conjugate nanoparticles
Wang, Yaoqi1; Wang, Xing1; Deng, Feiyang1; Zheng, Nan2; Liang, Yanqin1; Zhang, Hua1; He, Bing1; Dai, Wenbing1; Wang, Xueqing1; Zhang, Qiang1,3
通讯作者Wang, Xueqing(1)
关键词Doxorubicin conjugates Self-assembling nanoparticles Linker type Linker length Linkage site Anti-tumor efficiency
刊名JOURNAL OF CONTROLLED RELEASE
2018-06-10
DOI10.1016/j.jconrel.2018.04.019
279页:136-146
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]CANCER-THERAPY ; ENDOSOMAL ESCAPE ; DELIVERY ; PRODRUG ; RELEASE ; CHEMOTHERAPY ; PACLITAXEL ; CELLS ; REDOX ; NANOMEDICINES
英文摘要

Drug-drug conjugate nanoparticles (DDC NPs) is a potential method for overcoming poor solubility and nonspecific action in cancer therapy, which is based on its high drug loading efficiency and passive tumor-target properties. Our laboratory has prepared DOX-SS-DOX NPs based on disulfide-linked doxorubicin (DOX) drug-drug conjugate, which showed well physical stability and similar anti-tumor efficacy as liposomes. However, how structures of DDCs influence the self-assembling and anti-tumor efficacy is still seldom clarified and needs further investigation. Here, we discussed the role of linker types, length and linkage site in the NPs self-assembling and anti-tumor efficacy. A series of DOX prodrugs were prepared and all the prodrugs could selfassemble into NPs except DOX-SS-DOX (2), indicating the linker length played an important role during selfassembling process. The linkage sites and types of linker exhibited great influence on in vitro cytotoxicity and in vivo anti-tumor efficacy, particularly, modification on C-14 hydroxyl was more efficient for DOX release than on amino group. Besides, disulfide-bond was not cleaved and DOX-SH release did not occur in the metabolism process. The function of disulfide-bond was to enhance the release of DOX in the hydrolysis process. These findings is meaningful for effective prodrug NPs design for therapeutics.

语种英语
WOS记录号WOS:000433211300013
通讯作者邮箱wangxq@bjmu.edu.cn
第一作者单位Peking Univ, Sch Pharmaceut Sci, Beijing Key Lab Mol Pharmaceut, New Drug Delivery Syst, Beijing 100191, Peoples R China
通讯作者单位Peking Univ, Sch Pharmaceut Sci, Beijing Key Lab Mol Pharmaceut, New Drug Delivery Syst, Beijing 100191, Peoples R China
ISSN0168-3659
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/142183
专题北京大学药学院_天然药物与仿生药物国家重点实验室
北京大学药学院
北京大学药学院_药剂学系
北京大学口腔医学院_后勤综合协调处
北京大学临床肿瘤学院_乳腺癌预防治疗中心
作者单位1.Peking Univ, Sch Pharmaceut Sci, Beijing Key Lab Mol Pharmaceut, New Drug Delivery Syst, Beijing 100191, Peoples R China;
2.Peking Univ, Canc Hosp & Inst, Key Lab Carcinogenesis & Translat Res, Natl Drug Clin Trial Ctr,Minist Educ, Beijing 100142, Peoples R China;
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Wang, Yaoqi,Wang, Xing,Deng, Feiyang,et al. The effect of linkers on the self-assembling and anti-tumor efficacy of disulfide-linked doxorubicin drug-drug conjugate nanoparticles[J]. JOURNAL OF CONTROLLED RELEASE,2018,279:136-146.
APA Wang, Yaoqi.,Wang, Xing.,Deng, Feiyang.,Zheng, Nan.,Liang, Yanqin.,...&Zhang, Qiang.(2018).The effect of linkers on the self-assembling and anti-tumor efficacy of disulfide-linked doxorubicin drug-drug conjugate nanoparticles.JOURNAL OF CONTROLLED RELEASE,279,136-146.
MLA Wang, Yaoqi,et al."The effect of linkers on the self-assembling and anti-tumor efficacy of disulfide-linked doxorubicin drug-drug conjugate nanoparticles".JOURNAL OF CONTROLLED RELEASE 279(2018):136-146.
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