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

Author:
Wei, Bing, Tao, Yangyang, Wang, Xin, Tang, Rupei, Wang, Jun, Wang, Rui, Qiu, Liying
Source:
ACS Applied Materials & Interfaces 2015 v.7 no.19 pp. 10436-10445
ISSN:
1944-8252
Subject:
acute toxicity, adverse effects, amides, biocompatibility, composite polymers, condensation reactions, cytotoxicity, drug carriers, drug therapy, esters, fluorouracil, mice, neoplasms, oral administration, toxicity testing
Abstract:
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.
Agid:
5282894