Schmeltzer Robert C, Schmalenberg Kristine E, Uhrich Kathryn E
Department of Chemistry and Chemical Biology, Rutgers University, 610 Taylor Road, Piscataway, New Jersey 08854, USA.
Biomacromolecules. 2005 Jan-Feb;6(1):359-67. doi: 10.1021/bm049544+.
This paper describes the synthesis and cytotoxicity of poly(anhydride esters) that are composed of several salicylate derivatives, including halogenated salicylates, aminosalicylates, salicylsalicylic acid, and thiolsalicylic acid. The incorporation of these nonsteroidal antiinflammatory drugs (NSAIDs) into a biodegradable polymer backbone yields drug-based polymers that have potential for a variety of applications. The poly(anhydride esters) were synthesized by melt condensation polymerization. The halogenated salicylate derivatives yielded the highest molecular polymers as well as the highest glass transition temperatures. All polymers displayed in vitro degradation lag times from 1 to 3 days, depending on the water solubility of the salicylate derivative. Cell viability and proliferation were determined with L929 fibroblast cells in serum-containing medium to assess the polymer cytotoxicities, which varied as a function of the saliyclate chemistry. Cell morphology was normal for most of the polymers evaluated.
本文描述了由几种水杨酸酯衍生物组成的聚（酸酐酯）的合成及其细胞毒性，这些衍生物包括卤代水杨酸酯、氨基水杨酸酯、水杨酰水杨酸和硫代水杨酸。将这些非甾体抗炎药（NSAIDs）掺入可生物降解的聚合物主链中，得到了具有多种应用潜力的基于药物的聚合物。聚（酸酐酯）通过熔融缩聚法合成。卤代水杨酸酯衍生物得到了分子量最高的聚合物以及最高的玻璃化转变温度。所有聚合物在体外的降解滞后时间为1至3天，这取决于水杨酸酯衍生物的水溶性。在含血清培养基中用L929成纤维细胞测定细胞活力和增殖，以评估聚合物的细胞毒性，其随水杨酸酯化学组成的变化而变化。对于大多数评估的聚合物，细胞形态正常。
