‡Engineering Research Center for Biomedical Materials, School of Life Science, Anhui University, 111 Jiulong Road, Hefei, Anhui Province 230601, P. R. China.
§School of Pharmaceutical Science, Jiangnan University, 1800 Lihu Road, Wuxi, Jiangsu Province 214122, P. R. China.
ACS Appl Mater Interfaces. 2015 May 20;7(19):10436-45. doi: 10.1021/acsami.5b01687. Epub 2015 May 8.
Two new poly(ortho ester amide) copolymers (POEA-4 and POEA-5) were synthesized via polycondensation of a new ortho ester diamine monomer with active esters of different aliphatic diacids. The kinetics of POEA mass loss and release of 5-FU were both nearly zero-order, suggesting predominantly surface-restricted polymer erosion and drug release. In vitro cytotoxicity tests demonstrated that both copolymers have excellent biocompatibility. In vivo acute toxicity tests suggested that oral administration of POEA-4 and POEA-5 did not cause any adverse effects on mice even at a very high dose (2000 mg/kg). In vivo antitumor efficacy against H22 transplanted tumors of 5-FU-loaded POEA tablets were fully examined. We envision that, with further optimization, POEA-based materials could have great potential as drug carriers for oral chemotherapy.
两种新型聚（原酸酯酰胺）共聚物（POEA-4 和 POEA-5）通过新型邻酯二胺单体与不同脂肪族二酸的活性酯的缩聚反应合成。POEA 质量损失和 5-FU 释放的动力学均接近零级，表明主要是表面受限的聚合物侵蚀和药物释放。体外细胞毒性试验表明两种共聚物均具有良好的生物相容性。体内急性毒性试验表明，即使在很高的剂量（2000mg/kg）下，POEA-4 和 POEA-5 的口服给药也不会对小鼠造成任何不良影响。对载有 5-FU 的 POEA 片的 H22 移植瘤的体内抗肿瘤疗效进行了全面研究。我们设想，通过进一步优化，基于 POEA 的材料有可能成为口服化疗的药物载体。
