铂类药物偶联物的大分子设计

N. Koseva
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引用次数: 2

摘要

顺铂及其类似物具有毒理学不良、血液循环时间短、生物分布不特异性等缺点。此外,在生物液体中,顺铂被含氮和含硫的生物分子灭活。将药物偶联到水溶性聚合物上是一种提高治疗效率的可行方法。讨论了含羧酸的顺铂聚合物载体的实例以及大分子结构对共轭物行为的影响。
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Macromolecular Design of Platinum Drug Conjugates
Cisplatin and its analogues display common drawbacks such as unfavorable toxicological profile, short blood circulation time and non-specific bio-distribution. Besides that, in biological fluids cisplatin is inactivated by nitrogenand sulphur-containing biomolecules. Drug conjugation to a water soluble polymer is a feasible approach to enhance therapeutic efficiency. Examples of carboxylate-containing polymer carriers of cisplatin and the effect of macromolecular architecture on the behavior of conjugates are discussed.
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