Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy.
Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy.
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DOI：
10.3390/molecules201219804
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发表时间：
2015-12-04
期刊：
影响因子：
--
通讯作者：
Raucher D
中科院分区：
文献类型：
--
作者：
Dragojevic S;Ryu JS;Raucher D
大多数抗癌药物水溶性差，对健康组织产生不良影响，从而对癌症化疗的临床疗效和治疗安全性造成很大限制。为了帮助避免与溶解度相关的问题，大多数癌症药物现在都用助溶剂配制。然而，这些药物通常也会带来严重的副作用，从而限制有效的治疗和患者的生活质量。解决抗癌药物溶解度和选择性问题的一种有前途的方法是将它们与聚合物载体结合形成基于聚合物的前药。这些基于聚合物的前药是大分子载体，旨在增加抗肿瘤药物的水溶性，可以增强生物利用度。此外，基于聚合物的前药方法利用肿瘤生理学的独特特征来被动促进肿瘤内积累，从而改善化疗药物的药代动力学和药理学性质。这篇综述介绍了基于聚合物的前药的基本概念，概述了当前新兴的合成、天然和基因工程聚合物，这些聚合物目前在临床前或临床试验中提供抗癌药物，并强调了它们在抗癌治疗中的主要预期应用。
The majority of anticancer drugs have poor aqueous solubility, produce adverse effects in healthy tissue, and thus impose major limitations on both clinical efficacy and therapeutic safety of cancer chemotherapy. To help circumvent problems associated with solubility, most cancer drugs are now formulated with co-solubilizers. However, these agents often also introduce severe side effects, thereby restricting effective treatment and patient quality of life. A promising approach to addressing problems in anticancer drug solubility and selectivity is their conjugation with polymeric carriers to form polymer-based prodrugs. These polymer-based prodrugs are macromolecular carriers, designed to increase the aqueous solubility of antitumor drugs, can enhance bioavailability. Additionally, polymer-based prodrugs approach exploits unique features of tumor physiology to passively facilitate intratumoral accumulation, and so improve chemodrug pharmacokinetics and pharmacological properties. This review introduces basic concepts of polymer-based prodrugs, provides an overview of currently emerging synthetic, natural, and genetically engineered polymers that now deliver anticancer drugs in preclinical or clinical trials, and highlights their major anticipated applications in anticancer therapies.
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影响因子：
3.7
作者：
Bidwell GL 3rd;Perkins E;Hughes J;Khan M;James JR;Raucher D
通讯作者：
Raucher D
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影响因子：
14
作者：
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Luo, Juntao
影响因子：
5.8
作者：
Banerjee, T;Mitra, S;Maitra, A
通讯作者：
Maitra, A
影响因子：
3.1
作者：
Buckway B;Frazier N;Gormley AJ;Ray A;Ghandehari H
通讯作者：
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影响因子：
4.6
作者：
Chytil, Petr;Koziolova, Eva;Etrych, Tomas
通讯作者：
Etrych, Tomas