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.
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Authors | Guangxin Zhou, Xiaoyun Cheng, Sujia Wu, Xiqun Jiang, Xin Shi, Jiangning Chen, Junfeng Zhang, Jianning Zhao |
Journal | The 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 |
PMID | 22885620
(Publication Type: Journal Article)
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Chemical References |
- Antimetabolites, Antineoplastic
- PHEA-MTX conjugate
- Peptides
- Polymers
- Methotrexate
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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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