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探索聚合物缀合物在抗癌药物传递中的作用:当前趋势和未来展望。

Exploring the role of polymeric conjugates toward anti-cancer drug delivery: Current trends and future projections.

机构信息

Department of Pharmacy, Sarguja University, Ambikapur, Chhattisgarh 497001, India.

Rungta College of Pharmaceutical Sciences and Research, Bhilai, Chhattisgarh 490024, India.

出版信息

Int J Pharm. 2018 Sep 5;548(1):500-514. doi: 10.1016/j.ijpharm.2018.06.060. Epub 2018 Jun 28.

Abstract

Utilizing the diverse features of biocompatible polymers to target drugs into the tumor/s has been a research hotspot since last decade. Such polymeric conjugates of anti-cancer drugs have proven their potential in providing sustained release of drugs with reduced systemic toxicity and improved tumor retention. Polymers like polyethylene glycol (PEG), N-(2-Hydroxypropyl) methacrylamide (HPMA), Polylactic-co-glycolic acid (PLGA), Polyamidoamine (PAMAM), and others remain exploited for their specific as well as shared characteristics in the rational delivery of anti-cancer agents. Variable nano size, attachment with tumor-specific proteins, responsiveness to stimuli and ability to deliver a wide range of molecules like drugs, antibodies and peptides are some of the achievements of polymeric nano-conjugates so far. Many such conjugates have shown potential clinically which has attracted the researchers and promoted further advancements of the technique. Apart from achievements the polymeric conjugates suffer from shortcomings like poor drug loading and chances of potential chronic-systemic toxicities. The review highlights key findings of research in recent time and advancements taking place in the field of polymeric conjugates of anti-cancer drugs along with the limitations. We have also emphasized on newer and relatively less explored applications of tumor-targeted polymeric conjugates which can add new dimensions to this technique.

摘要

利用生物相容性聚合物的多种特性将药物靶向肿瘤/组织一直是过去十年的研究热点。这类抗癌药物的聚合物缀合物已被证明具有潜力,可提供药物的持续释放,减少全身毒性并提高肿瘤保留率。聚乙二醇(PEG)、N-(2-羟丙基)甲基丙烯酰胺(HPMA)、聚乳酸-羟基乙酸共聚物(PLGA)、聚酰胺胺(PAMAM)等聚合物因其在抗癌药物合理传递方面的独特和共同特性而被广泛利用。可变的纳米尺寸、与肿瘤特异性蛋白的结合、对刺激的响应能力以及能够递送广泛的分子,如药物、抗体和肽,是聚合物纳米缀合物迄今为止取得的一些成就。许多这样的缀合物在临床上已经显示出了潜力,这吸引了研究人员并促进了该技术的进一步发展。除了取得的成就外,聚合物缀合物还存在一些缺点,如药物载药量低和潜在的慢性全身性毒性的风险。本综述重点介绍了最近一段时间在抗癌药物聚合物缀合物领域的研究进展和取得的成果,以及存在的局限性。我们还强调了肿瘤靶向聚合物缀合物的一些新的和相对较少探索的应用,这可以为该技术增添新的维度。

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