Lactose targeting oxaliplatin prodrug loaded micelles for more effective chemotherapy of hepatocellular carcinoma
文献类型：期刊论文
| 作者 | Yang, Lixin1; Xiao, Haihua1,2; Yan, Lesan1,2; Wang, Rui1,2; Huang, Yubin1; Xie, Zhigang1; Jing, Xiabin1 |
| 刊名 | JOURNAL OF MATERIALS CHEMISTRY B
 |
| 出版日期 | 2014 |
| 卷号 | 2期号:15页码:2097-2106 |
| ISSN号 | 2050-750X |
| DOI | 10.1039/c3tb21709d |
| 英文摘要 | A sugar active targeting system for the platinum(IV) prodrug [oxaliplatin(IV)-COOH or in short form OxaPt(IV)] of clinically relevant oxaliplatin (OxaPt(II)) has been reported here for the first time. To achieve this, a series of hydrophilic biocompatible polyurethanes containing free pair-wised pendant amino groups (PU) were synthesized and then lactobionic acid (LA) was grafted to the polyurethane as a targeting moiety, in order to prepare PU-LA conjugates. Thereafter, the prodrug, OxaPt(IV) was introduced into the PU-LA conjugates resulting in the formation of polyurethane platinum(IV) conjugates (PU-LA/Pt) with targeting LA groups. Similarly, PU-Pt conjugates without the LA targeting groups were also prepared. These conjugates were self-assembled into micelles [non-targeting micelles: M(PU-Pt) and targeting micelles: M(PU-LA/Pt)] in water. An in vitro study demonstrated that, compared with M(PU-Pt), M(PU-LA/Pt) demonstrated a lower IC50 (79 mu M vs. 126 mu M) at 72 h and greater cellular uptake of drugs in HepG2 cells. An in vivo study revealed that M(PU-Pt) and M(PU-LA/Pt) displayed much higher blood drug concentrations and bioavailabilities than the free drug, OxaPt(IV). Moreover, M(PU-LA/Pt) showed enriched distribution in the liver and xenograft H22 tumors as well as better antitumor efficacy. M(PU-LA/ Pt) may be a promising polymeric prodrug of the widely used OxaPt(II) for the clinical treatment of various liver cancers. |
| 语种 | 英语 |
| WOS记录号 | WOS:000333095000005 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/50653]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Yang, Lixin |
| 作者单位 | 1.Chinese Acad Sci, Changchun Inst Appl Chem, State Key Lab Polymer Phys & Chem, Changchun 130022, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Lixin,Xiao, Haihua,Yan, Lesan,et al. Lactose targeting oxaliplatin prodrug loaded micelles for more effective chemotherapy of hepatocellular carcinoma[J]. JOURNAL OF MATERIALS CHEMISTRY B,2014,2(15):2097-2106. |
| APA | Yang, Lixin.,Xiao, Haihua.,Yan, Lesan.,Wang, Rui.,Huang, Yubin.,...&Jing, Xiabin.(2014).Lactose targeting oxaliplatin prodrug loaded micelles for more effective chemotherapy of hepatocellular carcinoma.JOURNAL OF MATERIALS CHEMISTRY B,2(15),2097-2106. |
| MLA | Yang, Lixin,et al."Lactose targeting oxaliplatin prodrug loaded micelles for more effective chemotherapy of hepatocellular carcinoma".JOURNAL OF MATERIALS CHEMISTRY B 2.15(2014):2097-2106. |
入库方式： OAI收割
来源：化学研究所
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