A poly(glycerol-sebacate-(5-fluorouracil-1-acetic acid)) polymer with potential use for cancer therapy

作者：Sun, Zhi-Jie^*; Sun, Bo; Sun, Cheng-Wu; Wang, Li-Bo; Xie, Xin; Ma, Wen-Chao; Lu, Xi-Li; Dong, De-Li

来源：Journal of Bioactive and Compatible Polymers, 2012, 27(1): 18-30.

DOI：10.1177/0883911511431876

• poly(glycerol-sebacate)
• poly(glycerol-sebacate-(5-fluorouracil-1-acetic acid))
• 5-fluorouracil
• 5-fluorouracil-1-acetic acid
• antitumor
• cancer therapy
• in vitro degradation
• in vivo degradation

In this study, 5-fluorouracil-1-acetic acid was chemically conjugated with poly(glycerol-sebacate) (PGS) to form a unitary polymer poly(glycerol-sebacate- (5-fluorouracil-1-acetic acid)) (PGS-5-FU-CH2COOH). The structure, the in vitro antitumor activity of 5-FU-CH2COOH, the in vitro degradation, the drug release, and antitumor activity as well as the in vivo degradation and tissue biocompatibility of PGS-5-FU-CH2COOH were investigated. The 5-FU-CH2COOH inhibited HeLa (human cervical cancer cell line) and SGC-7901 (human gastric adenocarcinoma cell line) tumor cells with a half maximal inhibitory concentration (IC50) of 0.196 and 0.267 mu M, respectively, after a 3-day incubation. The in vitro drug release profiles of PGS-5-FU-CH2COOH exhibited a biphasic release with an initial exponential phase in the first week and then the second constant linear phase. An in vitro antitumor assay of the PGS-5-FU-CH2COOH polymer showed significant cytotoxicity against tumor cells. The implanted PGS-5-FU-CH2COOH degraded completely in 1 month after implantation. The antitumor activity and improved drug release profile of PGS-5-FU-CH2COOH indicate its potential as an implantable polymer for cancer therapy.

• 出版日期2012-1
• 单位哈尔滨医科大学; 哈尔滨工程大学