Surface-Eroding Poly(ortho ester amides) for Highly Efficient Oral Chemotherapy

作者：Bing Wei, Yangyang Tao, Xin Wang, Rupei Tang, Jun Wang, Rui Wang, Liying Qiu · 发表于：ACS Applied Materials & Interfaces · 年份：2015 · DOI：10.1021/acsami.5b01687 · 被引用次数：51 · 研究领域：Dendrimers and Hyperbranched Polymers、Nanoparticle-Based Drug Delivery、Synthesis and properties of polymers

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.