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本文引用的文献

1
Synthesis and evaluation of a backbone biodegradable multiblock HPMA copolymer nanocarrier for the systemic delivery of paclitaxel.合成与评价一种主链可生物降解的多嵌段 HPMA 共聚物纳米载体用于紫杉醇的系统给药。
J Control Release. 2013 Feb 28;166(1):66-74. doi: 10.1016/j.jconrel.2012.12.009. Epub 2012 Dec 20.
2
Anti-CD20 multivalent HPMA copolymer-Fab' conjugates for the direct induction of apoptosis.抗 CD20 多价 HPMA 共聚物-Fab' 缀合物可直接诱导细胞凋亡。
Biomaterials. 2012 Oct;33(29):7174-81. doi: 10.1016/j.biomaterials.2012.06.024. Epub 2012 Jul 12.
3
HPMA copolymer-doxorubicin conjugates: The effects of molecular weight and architecture on biodistribution and in vivo activity.HPMA 共聚物-阿霉素偶联物：分子量和结构对体内分布和体内活性的影响。
J Control Release. 2012 Dec 28;164(3):346-54. doi: 10.1016/j.jconrel.2012.06.029. Epub 2012 Jun 30.
4
Biological activity of anti-CD20 multivalent HPMA copolymer-Fab' conjugates.抗 CD20 多价 HPMA 共聚物-Fab' 缀合物的生物学活性。
Biomacromolecules. 2012 Mar 12;13(3):727-35. doi: 10.1021/bm201656k. Epub 2012 Feb 21.
5
The journey of a drug-carrier in the body: an anatomo-physiological perspective.药物载体在体内的旅程：解剖生理学视角。
J Control Release. 2012 Jul 20;161(2):152-63. doi: 10.1016/j.jconrel.2011.09.098. Epub 2011 Oct 6.
6
Biodegradable Multiblock Poly[N-(2-hydroxypropyl)methacrylamide] via Reversible Addition-Fragmentation Chain Transfer Polymerization and Click Chemistry.通过可逆加成-断裂链转移聚合和点击化学制备可生物降解的多嵌段聚[N-(2-羟丙基)甲基丙烯酰胺]
Macromolecules. 2011 Apr 26;44(8):2481-2488. doi: 10.1021/ma102574e.
7
Synthesis of Biodegradable Multiblock Copolymers by Click Coupling of RAFT-Generated HeterotelechelicPolyHPMA Conjugates.通过RAFT生成的杂臂端基聚（N-（2-羟丙基）甲基丙烯酰胺）共轭物的点击偶联合成可生物降解的多嵌段共聚物。
React Funct Polym. 2011 Mar 1;71(3):294-302. doi: 10.1016/j.reactfunctpolym.2010.10.005.
8
Backbone degradable multiblock N-(2-hydroxypropyl)methacrylamide copolymer conjugates via reversible addition-fragmentation chain transfer polymerization and thiol-ene coupling reaction.通过可逆加成-断裂链转移聚合和硫醇-烯点击反应制备可降解多嵌段 N-(2-羟丙基)甲基丙烯酰胺共聚物偶联物。
Biomacromolecules. 2011 Jan 10;12(1):247-52. doi: 10.1021/bm101254e. Epub 2010 Dec 15.
9
Biomaterials and drug delivery: past, present, and future.生物材料与药物递送：过去、现在与未来。
Mol Pharm. 2010 Aug 2;7(4):922-5. doi: 10.1021/mp1001813.
10
The EPR effect: Unique features of tumor blood vessels for drug delivery, factors involved, and limitations and augmentation of the effect.EPR 效应：用于药物输送的肿瘤血管的独特特征、涉及的因素以及该效应的局限性和增强。
Adv Drug Deliv Rev. 2011 Mar 18;63(3):136-51. doi: 10.1016/j.addr.2010.04.009. Epub 2010 May 2.

长循环、主链可降解 HPMA 共聚物-阿霉素偶联物的合成及其分子量依赖性抗肿瘤活性评价。

Synthesis of long-circulating, backbone degradable HPMA copolymer-doxorubicin conjugates and evaluation of molecular-weight-dependent antitumor efficacy.

机构信息

Department of Pharmaceutics and Pharmaceutical Chemistry, University of Utah, Salt Lake City, Utah 84112, USA.

出版信息

Macromol Biosci. 2013 Feb;13(2):155-60. doi: 10.1002/mabi.201200353. Epub 2013 Jan 22.

DOI:10.1002/mabi.201200353
PMID:23339052
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4595041/
Abstract

Backbone degradable, linear, multiblock N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-doxorubicin (DOX) conjugates are synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization followed by chain extension via thiol-ene click reaction. The examination of molecular-weight-dependent antitumor activity toward human ovarian A2780/AD carcinoma in nude mice reveals enhanced activity of multiblock, second-generation, higher molecular weight conjugates when compared with traditional HPMA copolymer-DOX conjugates. The examination of body weight changes during treatment indicates the absence of non-specific adverse effects.

摘要

通过可逆加成-断裂链转移（RAFT）聚合合成了可降解、线性、多嵌段 N-（2-羟丙基）甲基丙烯酰胺（HPMA）共聚物-阿霉素（DOX）缀合物，然后通过硫醇-烯点击反应进行链延伸。在裸鼠中对人卵巢 A2780/AD 癌的分子量依赖性抗肿瘤活性的研究表明，与传统的 HPMA 共聚物-DOX 缀合物相比，多嵌段、第二代、更高分子量的缀合物具有增强的活性。在治疗过程中检查体重变化表明没有非特异性的不良反应。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a542/4595041/0ec0ebc95125/nihms726370f3.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a542/4595041/296939dee942/nihms726370f2.jpg
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