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Biodegradable Polymers from Aromatic β- Hydroxy Acids: From Medicinal Chemistry to Medical Device Applications

机译:来自芳族β-羟基酸的可生物降解的聚合物:从药用化学到医疗器械应用

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Biodegradable polymers (1) have gained attention in recent years because of their potential as drug carriers in medical device & pharmaceutical delivery technologies. Dr. Uhrich of Rutgers University contributed to the field by synthesizing several PolyNSAIDs (non-steroidal anti-inflammatory drug polymers). These polymers contain degradable ester and anhydride linkages which on erosion releases the active drug over a specific period. However, the melt polymerization methods used by Dr. Uhrich’s (2) produced low molecular weight polymers with poor mechanical properties that often resulted in bulk erosion. Because of the harsh polymerization conditions used in melt polymerization the method is not applicable to thermally labile drugs. Polymerix Corporation, which was founded originally based on Dr. Uhrich’s technology, has developed dehydrative coupling polymerization methods (3) that are milder and more efficient. Taking advantage of the newer synthetic methods, Polymerix developed a library of biodegradable PolyNSAIDs from salicylic acid, diflunisal and salsalate with a wider range of molecular weights and glass transitions and with a very high drug load of 70 to 90% by weight. The polymers synthesized by Polymerix’ solution methods exhibit Surface erosion (4) and release of the active drug in a controlled fashion. These advantages have led to the synthesis of new families of polymers that incorporate other pharmaceuticals directly into the polymer backbone.
机译:近年来,可生物降解的聚合物(1)在医疗器械和药物递送技术中作为药物载体的潜力,近年来受到关注。 Rutgers大学的Uhrich博士通过合成几种多牌剂(非甾体抗炎药物聚合物)贡献了该领域。这些聚合物含有可降解的酯和酸酐键,其在侵蚀上在特定时期释放活性药物。然而,Uhrich(2)博士使用的熔融聚合方法生产的低分子量聚合物,其机械性能差,其经常导致散装腐蚀。由于熔融聚合中使用的苛刻聚合条件,该方法不适用于热不稳定药物。最初基于Uhrich技术的技术成立的聚合物公司已经开发出脱水偶联聚合方法(3),较温和,更有效。利用更新的合成方法,聚合物开发了来自水杨酸,不同的分子量和玻璃化转变的可生物降解的多尔斯蛋白酶文库,具有较宽的分子量和玻璃转变,并且具有70至90重量%的非常高的药物负荷。由聚合物溶液方法合成的聚合物表现出表面侵蚀(4)并以受控的方式释放活性药物。这些优点导致了合成的新系列聚合物,其将其他药物直接掺入聚合物骨架中。

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