Preparation and antitumor activity of a polymeric derivative of methotrexate.

Guangxin Zhou, Xiaoyun Cheng, Sujia Wu, Xiqun Jiang, Xin Shi, Jiangning Chen, Junfeng Zhang, Jianning Zhao

Department of Orthopedics, Jinling Hospital, Nanjing, China.

The American journal of the medical sciences 2012 Oct

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A polymer-drug conjugate was developed by conjugating amino bonds of methotrexate (MTX) to succinoylated α,β-poly[(2-hydroxyethyl)-L-aspartamide] (PHEA). The therapeutic efficacy of PHEA-MTX was evaluated in vitro and in vivo. PHEA-MTX showed sustained release properties when incubated in pH 5.5 and pH 7.4 buffering solutions at 37°C. PHEA-MTX induced MG63 cell apoptosis in a time-dependent and concentration-dependent manner in vitro and inhibited the growth of S180 sarcoma in vivo. PHEA-MTX was more potent and, more importantly, displayed less systemic toxicity than free MTX. The enhanced therapeutic effects of PHEA-MTX suggest that the PHEA-MTX conjugate may have a greater potential for chemotherapy of cancers.

Citation

Guangxin Zhou, Xiaoyun Cheng, Sujia Wu, Xiqun Jiang, Xin Shi, Jiangning Chen, Junfeng Zhang, Jianning Zhao. Preparation and antitumor activity of a polymeric derivative of methotrexate. The American journal of the medical sciences. 2012 Oct;344(4):294-9