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首页> 外文期刊>RSC Advances >Synthesis and characterization of a poly(ethylene glycol)-poly(simvastatin) diblock copolymer
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Synthesis and characterization of a poly(ethylene glycol)-poly(simvastatin) diblock copolymer

机译：聚乙二醇-辛伐他汀二嵌段共聚物的合成与表征

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摘要

Biodegradable polyesters are commonly used as drug delivery vehicles, but their role is typically passive, and encapsulation approaches have limited drug payload. An alternative drug delivery method is to polymerize the active agent or its precursor into a degradable polymer. The prodrug simvastatin contains a lactone ring that lends itself to ring-opening polymerization (ROP). Consequently, simvastatin polymerization was initiated with 5 kDa monomethyl ether poly(ethylene glycol) (mPEG) and catalyzed via stannous octoate. Melt condensation reactions produced a 9.5 kDa copolymer with a polydispersity index of 1.1 at 150 degrees C up to a 75 kDa copolymer with an index of 6.9 at 250 degrees C. Kinetic analysis revealed first-order propagation rates. Infrared spectroscopy of the copolymer showed carboxylic and methyl ether stretches unique to simvastatin and mPEG, respectively. Slow degradation was demonstrated in neutral and alkaline conditions. Lastly, simvastatin, simvastatin-incorporated molecules, and mPEG were identified as the degradation products released. The present results show the potential of using ROP to polymerize lactone-containing drugs such as simvastatin.
机译：可生物降解的聚酯通常用作药物输送载体，但它们的作用通常是被动的，并且封装方法的药物有效载荷有限。另一种药物递送方法是将活性剂或其前体聚合成可降解的聚合物。辛伐他汀前药含有一个内酯环，可促进开环聚合（ROP）。因此，辛伐他汀聚合反应由5 kDa单甲基醚聚（乙二醇）（mPEG）引发，并通过辛酸亚锡催化。熔融缩合反应产生9.5kDa的共聚物，其在150℃下的多分散指数为1.1，直至75kDa的共聚物在250℃下的指数为6.9。动力学分析显示一阶传播速率。共聚物的红外光谱显示辛伐他汀和mPEG分别具有独特的羧基和甲基醚延伸率。在中性和碱性条件下显示出缓慢的降解。最后，辛伐他汀，包含辛伐他汀的分子和mPEG被确定为释放的降解产物。目前的结果表明使用ROP聚合含内酯的药物（如辛伐他汀）的潜力。

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