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

Wei, Bing, Tao, Yangyang, Wang, Xin, Tang, Rupei, Wang, Jun, Wang, Rui, Qiu, Liying
ACS Applied Materials & Interfaces 2015 v.7 no.19 pp. 10436-10445
acute toxicity, adverse effects, amides, biocompatibility, composite polymers, condensation reactions, cytotoxicity, drug carriers, drug therapy, esters, fluorouracil, mice, neoplasms, oral administration, toxicity testing
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.