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抗肿瘤聚合物疗法的临床进展

Clinical developments of antitumor polymer therapeutics.

作者信息

Parveen Shazia, Arjmand Farukh, Tabassum Sartaj

机构信息

Chemistry Department, Faculty of Science, Taibah University Yanbu Branch 46423 Yanbu Saudi Arabia

Department of Chemistry, Aligarh Muslim University Aligarh-202002 India.

出版信息

RSC Adv. 2019 Aug 8;9(43):24699-24721. doi: 10.1039/c9ra04358f.

Abstract

Polymer therapeutics encompasses polymer-drug conjugates that are nano-sized, multicomponent constructs already in the clinic as antitumor compounds, either as single agents or in combination with other organic drug scaffolds. Nanoparticle-based polymer-conjugated therapeutics are poised to become a leading delivery strategy for cancer treatments as they exhibit prolonged half-life, higher stability and selectivity, water solubility, longer clearance time, lower immunogenicity and antigenicity and often also specific targeting to tissues or cells. Compared to free drugs, polymer-tethered drugs preferentially accumulate in the tumor sites unlike conventional chemotherapy which does not discriminate between the cancer cells and healthy cells, thereby causing severe side-effects. It is also desirable that the drug reaches its site of action at a particular concentration and the therapeutic dose remains constant over a sufficiently long period of time. This can be achieved by opting for new formulations possessing polymeric systems of drug carriers. However, many challenges still remain unanswered in polymeric drug conjugates which need to be readdressed and therefore, can broaden the scope of this field. This review highlights some of the antitumor polymer therapeutics including polymer-drug conjugates, polymeric micelles, polymeric liposomes and other polymeric nanoparticles that are currently under investigation.

摘要

聚合物疗法包括聚合物-药物偶联物,它们是纳米级的多组分构建体,作为抗肿瘤化合物已进入临床,可作为单一药物或与其他有机药物支架联合使用。基于纳米颗粒的聚合物偶联疗法有望成为癌症治疗的主要递送策略,因为它们具有半衰期延长、稳定性和选择性更高、水溶性好、清除时间长、免疫原性和抗原性低等特点,并且通常还能特异性靶向组织或细胞。与游离药物相比,聚合物连接的药物优先在肿瘤部位蓄积,这与传统化疗不同,传统化疗不会区分癌细胞和健康细胞,从而导致严重的副作用。此外,药物以特定浓度到达其作用部位且治疗剂量在足够长的时间内保持恒定也是理想的。这可以通过选择具有药物载体聚合物系统的新制剂来实现。然而,聚合物药物偶联物中仍有许多挑战尚未得到解决,需要重新审视,因此这可以拓宽该领域的范围。本综述重点介绍了一些目前正在研究的抗肿瘤聚合物疗法,包括聚合物-药物偶联物、聚合物胶束、聚合物脂质体和其他聚合物纳米颗粒。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/07e0/9069890/1c4707036992/c9ra04358f-f1.jpg

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