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Tunable drug release profiles from salicylate-based poly(anhydride-ester) matrices using small molecule admixtures
Journal of Bioactive and Compatible Polymers ( IF 2.1 ) Pub Date : 2012-11-01 , DOI: 10.1177/0883911512464605
Michelle A Ouimet 1 , Sabrina S Snyder , Kathryn E Uhrich
Affiliation  

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.

中文翻译:


使用小分子混合物从水杨酸盐基聚(酸酐酯)基质中调节药物释放曲线



聚(酸酐酯)与水杨酸(一种非甾体类抗炎药)化学结合到聚合物主链中,提供高固有载药量。这些聚(酸酐酯)会在较长时间(>30 天)内水解降解释放水杨酸;然而,没有观察到水杨酸释放的初始滞后期。在需要立即释放水杨酸的应用中,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(酸酐酯)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、较大的水杨酸前药以及两者的 1:1 组合进行物理混合,分别为 1%、5% 和 10% (w/w)。与单独的聚合物相比,所有混合物都会立即释放水杨酸并降低玻璃化转变温度。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立即且恒定的水杨酸释放曲线。
更新日期:2012-11-01
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