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首页> 外文期刊>Acta biomaterialia >A complex of cyclohexane-1,2-diaminoplatinum with an amphiphilic biodegradable polymer with pendant carboxyl groups
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A complex of cyclohexane-1,2-diaminoplatinum with an amphiphilic biodegradable polymer with pendant carboxyl groups

机译：环己烷-1,2-二氨基铂与具有羧基侧基的两亲生物可降解聚合物的配合物

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摘要

A biodegradable and amphiphilic copolymer, MPEG-b-P(LA-co-MCC), which contains pendant carboxyl groups, was chosen as a drug carrier for the active anticancer part (DACH-Pt) of oxaliplatin to form an MPEG-b-P(LA-co-MCC/Pt) complex. It was able to self-assemble into micelles with a mean diameter of 30-40 nm, and a surface potential near -10 mV. The typical platinum content was 10 wt.%. The micelles showed acid-responsive drug release kinetics, which is beneficial for drug release in the intracellular environment. The Pt(II) species were released mainly in the form of DACH-Pt-Cl 2 in 150 mM NaCl solution and DACH-Pt 2+-(H 2O) 2 in pure water according to the results obtained by high-performance liquid chromatography coupled with inductively coupled plasma mass spectrometry and X-ray photoelectron spectroscopy. In vitro evaluation showed that the micelles displayed the same or higher cytotoxicities against SKOV-3, HeLa, and EC-109 cancer cells compared with oxaliplatin. The enhanced cytotoxicity against SKOV-3 cells is attributed to effective internalization of the micelles by the cells via endocytosis and the sensitivity of SKOV-3 cells to platinum drugs. This novel biodegradable and amphiphilic copolymer-based platinum drug will have great potential application in clinical use.
机译：选择含有羧基侧基的可生物降解的两亲共聚物MPEG-bP（LA-co-MCC）作为奥沙利铂的活性抗癌部分（DACH-Pt）的药物载体，以形成MPEG-bP（LA- co-MCC / Pt）复合物。它能够自组装成平均直径为30-40 nm，表面电势接近-10 mV的胶束。典型的铂含量为10重量％。胶束显示出酸响应的药物释放动力学，这对于细胞内环境中的药物释放是有益的。根据高效液相色谱法获得的结果，Pt（II）物质主要以在150 mM NaCl溶液中的DACH-Pt-Cl 2和在纯水中的DACH-Pt 2 +-（H 2O）2的形式释放。加上电感耦合等离子体质谱和X射线光电子能谱。体外评估表明，与奥沙利铂相比，胶束对SKOV-3，HeLa和EC-109癌细胞具有相同或更高的细胞毒性。针对SKOV-3细胞的增强的细胞毒性归因于细胞通过内吞作用使胶束有效内在化，以及SKOV-3细胞对铂药物的敏感性。这种新型的可生物降解且基于两亲共聚物的铂药物将在临床应用中具有巨大的潜在应用。

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