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Preparation and antitumor activity of a polymeric derivative of methotrexate.

Abstract
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.
AuthorsGuangxin Zhou, Xiaoyun Cheng, Sujia Wu, Xiqun Jiang, Xin Shi, Jiangning Chen, Junfeng Zhang, Jianning Zhao
JournalThe American journal of the medical sciences (Am J Med Sci) Vol. 344 Issue 4 Pg. 294-9 (Oct 2012) ISSN: 1538-2990 [Electronic] United States
PMID22885620 (Publication Type: Journal Article)
Chemical References
  • Antimetabolites, Antineoplastic
  • PHEA-MTX conjugate
  • Peptides
  • Polymers
  • Methotrexate
Topics
  • Antimetabolites, Antineoplastic (adverse effects, therapeutic use)
  • Cell Line, Tumor
  • Humans
  • Methotrexate (adverse effects, analogs & derivatives, therapeutic use)
  • Osteosarcoma (drug therapy)
  • Peptides
  • Polymers

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