Tunable drug release profiles from salicylate-based poly(anhydride-ester) matrices using small molecule admixtures.
Tunable drug release profiles from salicylate-based poly(anhydride-ester) matrices using small molecule admixtures.
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DOI：
10.1177/0883911512464605
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发表时间：
2012-11-01
影响因子：
1.7
通讯作者：
Uhrich KE
中科院分区：
文献类型：
--
作者：
Ouimet MA;Snyder SS;Uhrich KE
具有水杨酸（一种非甾体抗炎药）的聚（安替洛尔-酯）以化学方式并入聚合物主链中提供高固有药物负载。这些聚（己二酸酯-酯）在延长的时间段（>30天）内水解降解以释放水杨酸;然而，观察到没有水杨酸释放的初始滞后期。在需要水杨酸立即释放的应用中，该滞后期可能是不利的。将具有短（2天）和长（11天）滞后期的聚（己二酸酯-酯）与各种小分子混合，作为缩短或消除滞后期的手段。将水杨酸、较大的水杨酸前药和两者的1：1组合以各自1%、5%和10%（w/w）物理混合。与单独聚合物相比，所有混合物导致水杨酸立即释放和玻璃化转变温度降低。通过改变掺入聚合物基质中的水杨酸和水杨酸前药的量，实现了在不同时间段内的即时和恒定的水杨酸释放曲线。
Poly(anhydride-esters) with salicylic acid, a nonsteroidal anti-inflammatory drug, chemically incorporated into the polymer backbone provide high inherent drug loading. These poly(anhydride-esters) hydrolytically degrade to release salicylic acid over extended time periods (>30 days); however, an initial lag period of no salicylic acid release is observed. This lag period could be unfavorable in applications where immediate salicylic acid release is desired. Poly(anhydride-esters) with short (2 days) and long (11 days) lag periods were admixed with various small molecules as a means to shorten or eliminate the lag period. Salicylic acid, larger salicylic acid prodrugs, and 1:1 combinations of the two were physically admixed, each at 1%, 5%, and 10% (w/w). All admixtures resulted in immediate salicylic acid release and a decrease in glass transition temperatures compared to polymer alone. By varying the amounts of salicylic acid and salicylic acid prodrugs incorporated into the polymer matrix, immediate and constant salicylic acid release profiles over varied time periods were achieved.
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