具有弹性体特性和药物载体功能的可降解生物材料

B.I Dahiyat, E.M Posadas, S Hirosue, E Hostin, K.W Leong
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引用次数: 14

摘要

介绍了基于聚磷酸酯-聚氨酯(PPUs)的载药弹性体的设计。以二(2-羟基乙基)亚磷酸酯和二(6-羟基己基)亚磷酸酯为扩链剂,1,4-丁烷二异氰酸酯为硬段的基础。PPU主链上不稳定的磷酸酯键赋予聚合物可生物降解性。利用ppu中的活性亚磷酸酯侧链,对氨基水杨酸和苯佐卡因在有或没有间隔剂的情况下悬垂地附着在聚合物上。两种药物的体外释放在几个小时内完成。相比之下,加入到聚合物骨架中的乙胺丁醇在10多天内被释放出来。初步评估了药物载体对巨噬细胞系的细胞毒性。
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Degradable biomaterials with elastomeric characteristics and drug-carrier function

The design of drug-carrying elastomers based on poly(phosphoester-urethanes) (PPUs) is presented. Bis(2-hydroxyethyl)phosphite and bis(6-hydroxyhexyl)phosphite were used as the chain extenders and 1,4-butane diisocyanate was the basis of the hard segment. The labile phosphoester linkage in the backbone of the PPU confers biodegradability on the polymer. Using the reactive phosphite side chain in the PPUs, p-aminosalicylic acid and benzocaine were attached pendantly to the polymer with or without a spacer. In vitro release of both drugs was complete in several hours. In contrast, ethambutol incorporated into the backbone of the polymer was released in over 10 days. Preliminary cytotoxicity of the drug-carrier to a macrophage cell line was also assessed.

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